{"id":"https://openalex.org/W3205225556","doi":"https://doi.org/10.1021/acs.jmedchem.1c00681","title":"Development of 2-(5,6,7-Trifluoro-1H-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer","display_name":"Development of 2-(5,6,7-Trifluoro-1H-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer","publication_year":2021,"publication_date":"2021-10-18","ids":{"openalex":"https://openalex.org/W3205225556","doi":"https://doi.org/10.1021/acs.jmedchem.1c00681","mag":"3205225556","pmid":"https://pubmed.ncbi.nlm.nih.gov/34661404"},"language":"en","primary_location":{"id":"doi:10.1021/acs.jmedchem.1c00681","doi":"https://doi.org/10.1021/acs.jmedchem.1c00681","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.jmedchem.1c00681","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5107336789","display_name":"Eric Leblanc","orcid":"https://orcid.org/0000-0003-1838-7277","observed_orcids":["https://orcid.org/0000-0003-1838-7277"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Eric Leblanc","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5064411392","display_name":"Fuqiang Ban","orcid":"https://orcid.org/0000-0001-7950-433X","observed_orcids":["https://orcid.org/0000-0001-7950-433X"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Fuqiang Ban","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5063101101","display_name":"Ay\u015fe Derya Cavga","orcid":"https://orcid.org/0000-0001-5017-5042","observed_orcids":["https://orcid.org/0000-0001-5017-5042"]},"institutions":[{"id":"https://openalex.org/I1351752","display_name":"Ko\u00e7 University","ror":"https://ror.org/00jzwgz36","country_code":"TR","type":"education","lineage":["https://openalex.org/I1351752"]}],"countries":["TR"],"is_corresponding":false,"raw_author_name":"Ayse Derya Cavga","raw_affiliation_strings":["School of Medicine, Ko\u00e7 University, Rumelifeneri Yolu, Istanbul 34450, Turkey"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"School of Medicine, Ko\u00e7 University, Rumelifeneri Yolu, Istanbul 34450, Turkey","institution_ids":["https://openalex.org/I1351752"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5011615044","display_name":"Samuel O. Lawn","orcid":"https://orcid.org/0009-0005-8033-6990","observed_orcids":["https://orcid.org/0009-0005-8033-6990"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Sam Lawn","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5009207752","display_name":"Chia-Chi Flora Huang","orcid":"https://orcid.org/0000-0002-2150-3139","observed_orcids":["https://orcid.org/0000-0002-2150-3139"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Chia-Chi Flora Huang","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111817314","display_name":"Sankar Mohan","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I18014758","display_name":"Simon Fraser University","ror":"https://ror.org/0213rcc28","country_code":"CA","type":"education","lineage":["https://openalex.org/I18014758"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Sankar Mohan","raw_affiliation_strings":["Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada","institution_ids":["https://openalex.org/I18014758"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5056291527","display_name":"Matthew E.K. Chang","orcid":"https://orcid.org/0000-0001-5859-388X","observed_orcids":["https://orcid.org/0000-0001-5859-388X"]},"institutions":[{"id":"https://openalex.org/I165690674","display_name":"Oregon Health & Science University","ror":"https://ror.org/009avj582","country_code":"US","type":"education","lineage":["https://openalex.org/I165690674"]},{"id":"https://openalex.org/I4390039369","display_name":"OHSU Knight Cancer Institute","ror":"https://ror.org/002shna07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Matthew E. K. Chang","raw_affiliation_strings":["Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States","institution_ids":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5049232635","display_name":"Mark R. Flory","orcid":"https://orcid.org/0000-0002-6174-2708","observed_orcids":["https://orcid.org/0000-0002-6174-2708"]},"institutions":[{"id":"https://openalex.org/I165690674","display_name":"Oregon Health & Science University","ror":"https://ror.org/009avj582","country_code":"US","type":"education","lineage":["https://openalex.org/I165690674"]},{"id":"https://openalex.org/I4390039369","display_name":"OHSU Knight Cancer Institute","ror":"https://ror.org/002shna07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Mark R. Flory","raw_affiliation_strings":["Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States","institution_ids":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5039503529","display_name":"Fariba Ghaidi","orcid":"https://orcid.org/0009-0002-8664-7894","observed_orcids":["https://orcid.org/0009-0002-8664-7894"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Fariba Ghaidi","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5069316023","display_name":"Shreyas Lingadahalli","orcid":"https://orcid.org/0000-0002-9609-6486","observed_orcids":["https://orcid.org/0000-0002-9609-6486"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Shreyas Lingadahalli","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100389268","display_name":"Gang Chen","orcid":"https://orcid.org/0000-0002-4864-1451","observed_orcids":["https://orcid.org/0000-0002-4864-1451","https://orcid.org/0000-0003-2402-2987","https://orcid.org/0000-0002-8105-2384"]},"institutions":[{"id":"https://openalex.org/I18014758","display_name":"Simon Fraser University","ror":"https://ror.org/0213rcc28","country_code":"CA","type":"education","lineage":["https://openalex.org/I18014758"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Gang Chen","raw_affiliation_strings":["Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada","institution_ids":["https://openalex.org/I18014758"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5017835077","display_name":"Ivan Pak Lok Yu","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Ivan Pak Lok Yu","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5113588847","display_name":"H\u00e9l\u00e8ne Morin","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"H\u00e9l\u00e8ne Morin","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5090453688","display_name":"Nada Lallous","orcid":"https://orcid.org/0000-0002-8665-8641","observed_orcids":["https://orcid.org/0000-0002-8665-8641"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Nada Lallous","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5062125605","display_name":"Martin Edwin Gleave","orcid":"https://orcid.org/0000-0003-4235-0167","observed_orcids":["https://orcid.org/0000-0003-4235-0167"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Martin E. Gleave","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5009257291","display_name":"Hisham Mohammed","orcid":"https://orcid.org/0000-0003-0275-9793","observed_orcids":["https://orcid.org/0000-0003-0275-9793"]},"institutions":[{"id":"https://openalex.org/I165690674","display_name":"Oregon Health & Science University","ror":"https://ror.org/009avj582","country_code":"US","type":"education","lineage":["https://openalex.org/I165690674"]},{"id":"https://openalex.org/I4390039369","display_name":"OHSU Knight Cancer Institute","ror":"https://ror.org/002shna07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Hisham Mohammed","raw_affiliation_strings":["Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Knight Cancer Institute, Oregon Health & Science University, 3181 S.W. Sam Jackson Park Road, Portland, Oregon 97239, United States","institution_ids":["https://openalex.org/I165690674","https://openalex.org/I4390039369"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5063566841","display_name":"Robert Norman Young","orcid":"https://orcid.org/0000-0002-8235-6080","observed_orcids":["https://orcid.org/0000-0002-8235-6080"]},"institutions":[{"id":"https://openalex.org/I18014758","display_name":"Simon Fraser University","ror":"https://ror.org/0213rcc28","country_code":"CA","type":"education","lineage":["https://openalex.org/I18014758"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Robert N. Young","raw_affiliation_strings":["Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Simon Fraser University, 8888 University Drive, Burnaby, British Columbia V5A 1S6, Canada","institution_ids":["https://openalex.org/I18014758"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5113514052","display_name":"Paul S. Rennie","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Paul S. Rennie","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5016346851","display_name":"Nathan A. Lack","orcid":"https://orcid.org/0000-0001-7399-5844","observed_orcids":["https://orcid.org/0000-0001-7399-5844"]},"institutions":[{"id":"https://openalex.org/I1351752","display_name":"Ko\u00e7 University","ror":"https://ror.org/00jzwgz36","country_code":"TR","type":"education","lineage":["https://openalex.org/I1351752"]},{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA","TR"],"is_corresponding":true,"raw_author_name":"Nathan A. Lack","raw_affiliation_strings":["School of Medicine, Ko\u00e7 University, Rumelifeneri Yolu, Istanbul 34450, Turkey","Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":"https://orcid.org/0000-0001-7399-5844","affiliations":[{"raw_affiliation_string":"School of Medicine, Ko\u00e7 University, Rumelifeneri Yolu, Istanbul 34450, Turkey","institution_ids":["https://openalex.org/I1351752"]},{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5070580886","display_name":"Artem R Cherkasov","orcid":"https://orcid.org/0000-0002-1599-1439","observed_orcids":["https://orcid.org/0000-0002-1599-1439"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]},{"id":"https://openalex.org/I4405261103","display_name":"Vancouver Prostate Centre","ror":"https://ror.org/04skhpe58","country_code":"CA","type":"healthcare","lineage":["https://openalex.org/I4405261103"]}],"countries":["CA"],"is_corresponding":true,"raw_author_name":"Artem Cherkasov","raw_affiliation_strings":["Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada"],"raw_orcid":"https://orcid.org/0000-0002-1599-1439","affiliations":[{"raw_affiliation_string":"Vancouver Prostate Centre, University of British Columbia, 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada","institution_ids":["https://openalex.org/I141945490","https://openalex.org/I4405261103"]}]}],"institutions":[],"countries_distinct_count":3,"institutions_distinct_count":6,"corresponding_author_ids":["https://openalex.org/A5016346851","https://openalex.org/A5070580886"],"corresponding_institution_ids":["https://openalex.org/I1351752","https://openalex.org/I141945490","https://openalex.org/I4405261103"],"apc_list":{"value":5000,"currency":"USD","value_usd":5000},"apc_paid":null,"fwci":0.8694,"has_fulltext":false,"cited_by_count":13,"citation_normalized_percentile":{"value":0.67134735,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":95,"max":98},"biblio":{"volume":"64","issue":"20","first_page":"14968","last_page":"14982"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10543","display_name":"Prostate Cancer Treatment and Research","score":0.9984999895095825,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10543","display_name":"Prostate Cancer Treatment and Research","score":0.9984999895095825,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.00039999998989515007,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}},{"id":"https://openalex.org/T12534","display_name":"Protein Degradation and Inhibitors","score":0.00019999999494757503,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/castration-resistant-prostate-cancer","display_name":"castration-resistant prostate cancer","score":0.9129999876022339},{"id":"https://openalex.org/keywords/androgen-receptor","display_name":"androgen receptor","score":0.9909999966621399},{"id":"https://openalex.org/keywords/androgen-receptor-antagonists","display_name":"androgen receptor antagonists","score":0.7260000109672546},{"id":"https://openalex.org/keywords/enzalutamide-resistance","display_name":"enzalutamide resistance","score":0.8100000023841858},{"id":"https://openalex.org/keywords/androgen-deprivation-therapy","display_name":"androgen deprivation therapy","score":0.7009999752044678},{"id":"https://openalex.org/keywords/prodrugs","display_name":"prodrugs","score":0.6240000128746033},{"id":"https://openalex.org/keywords/oral-bioavailability","display_name":"oral bioavailability","score":0.871999979019165},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.7170000076293945},{"id":"https://openalex.org/keywords/coregulator-recruitment","display_name":"coregulator recruitment","score":0.6909999847412109},{"id":"https://openalex.org/keywords/chromatin-binding","display_name":"chromatin binding","score":0.7089999914169312},{"id":"https://openalex.org/keywords/prostate-specific-antigen","display_name":"prostate-specific antigen","score":0.6510000228881836}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.7594233751296997},{"id":"https://openalex.org/C61367390","wikidata":"https://www.wikidata.org/wiki/Q416601","display_name":"Androgen receptor","level":4,"score":0.7562617659568787},{"id":"https://openalex.org/C2776551883","wikidata":"https://www.wikidata.org/wiki/Q1996756","display_name":"Enzalutamide","level":5,"score":0.7427487373352051},{"id":"https://openalex.org/C2780192828","wikidata":"https://www.wikidata.org/wiki/Q181257","display_name":"Prostate cancer","level":3,"score":0.682387113571167},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.6425334215164185},{"id":"https://openalex.org/C108215921","wikidata":"https://www.wikidata.org/wiki/Q603741","display_name":"Prodrug","level":2,"score":0.6137155294418335},{"id":"https://openalex.org/C2778327999","wikidata":"https://www.wikidata.org/wiki/Q188777","display_name":"Carboxamide","level":2,"score":0.5965398550033569},{"id":"https://openalex.org/C2779322244","wikidata":"https://www.wikidata.org/wiki/Q574820","display_name":"Antiandrogen","level":4,"score":0.5143510103225708},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.43415600061416626},{"id":"https://openalex.org/C2777911890","wikidata":"https://www.wikidata.org/wiki/Q62614","display_name":"Androgen","level":3,"score":0.3915211260318756},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.25479423999786377},{"id":"https://openalex.org/C126322002","wikidata":"https://www.wikidata.org/wiki/Q11180","display_name":"Internal medicine","level":1,"score":0.20967960357666016},{"id":"https://openalex.org/C121608353","wikidata":"https://www.wikidata.org/wiki/Q12078","display_name":"Cancer","level":2,"score":0.2001030147075653},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.11690250039100647},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.11168161034584045},{"id":"https://openalex.org/C71315377","wikidata":"https://www.wikidata.org/wiki/Q11364","display_name":"Hormone","level":2,"score":0.10071152448654175},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D000076722","descriptor_name":"Drug Development","qualifier_ui":null,"qualifier_name":null,"is_major_topic":true},{"descriptor_ui":"D000284","descriptor_name":"Administration, Oral","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000726","descriptor_name":"Androgen Antagonists","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D000726","descriptor_name":"Androgen Antagonists","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D000726","descriptor_name":"Androgen Antagonists","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D001682","descriptor_name":"Biological Availability","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D002470","descriptor_name":"Cell Survival","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":false},{"descriptor_ui":"D004305","descriptor_name":"Dose-Response Relationship, Drug","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D004354","descriptor_name":"Drug Screening Assays, Antitumor","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008297","descriptor_name":"Male","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008958","descriptor_name":"Models, Molecular","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D011944","descriptor_name":"Receptors, Androgen","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D015394","descriptor_name":"Molecular Structure","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D045744","descriptor_name":"Cell Line, Tumor","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D049109","descriptor_name":"Cell Proliferation","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":false},{"descriptor_ui":"D064129","descriptor_name":"Prostatic Neoplasms, Castration-Resistant","qualifier_ui":"Q000188","qualifier_name":"drug therapy","is_major_topic":true},{"descriptor_ui":"D064129","descriptor_name":"Prostatic Neoplasms, Castration-Resistant","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D064129","descriptor_name":"Prostatic Neoplasms, Castration-Resistant","qualifier_ui":"Q000473","qualifier_name":"pathology","is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/acs.jmedchem.1c00681","doi":"https://doi.org/10.1021/acs.jmedchem.1c00681","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.jmedchem.1c00681","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmid:34661404","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/34661404","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of medicinal chemistry","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.98580002784729,"id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[{"id":"https://openalex.org/G2052260643","display_name":null,"funder_award_id":"272111","funder_id":"https://openalex.org/F4320334506","funder_display_name":"Canadian Institutes of Health Research"},{"id":"https://openalex.org/G296494197","display_name":null,"funder_award_id":"SP2013-02","funder_id":"https://openalex.org/F4320319921","funder_display_name":"Prostate Cancer Canada"},{"id":"https://openalex.org/G739786069","display_name":null,"funder_award_id":"390757","funder_id":"https://openalex.org/F4320334506","funder_display_name":"Canadian Institutes of Health Research"},{"id":"https://openalex.org/G7835445324","display_name":null,"funder_award_id":"701585","funder_id":"https://openalex.org/F4320334576","funder_display_name":"Canadian Cancer Society Research Institute"},{"id":"https://openalex.org/G8311765774","display_name":"DEVELOPEMNT OF NOVEL DRUGS THAT TARGET COACTIVATION SITES OF THE ANDROGEN RESEPTOR FOR TREATMENT OF ANTIANDROGEN0RESISTANT PROSTATE CANCER","funder_award_id":"W81XWH1210401","funder_id":"https://openalex.org/F4320306078","funder_display_name":"U.S. Department of Defense"}],"funders":[{"id":"https://openalex.org/F4320306078","display_name":"U.S. Department of Defense","ror":"https://ror.org/0447fe631"},{"id":"https://openalex.org/F4320319921","display_name":"Prostate Cancer Canada","ror":"https://ror.org/03p641z80"},{"id":"https://openalex.org/F4320334506","display_name":"Canadian Institutes of Health Research","ror":"https://ror.org/01gavpb45"},{"id":"https://openalex.org/F4320334576","display_name":"Canadian Cancer Society Research Institute","ror":"https://ror.org/017343w90"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":42,"referenced_works":["https://openalex.org/W1948562438","https://openalex.org/W1981652396","https://openalex.org/W2006138763","https://openalex.org/W2017184248","https://openalex.org/W2018556051","https://openalex.org/W2030283358","https://openalex.org/W2035503835","https://openalex.org/W2055655957","https://openalex.org/W2059097089","https://openalex.org/W2059183805","https://openalex.org/W2076235446","https://openalex.org/W2091098941","https://openalex.org/W2091710329","https://openalex.org/W2095722179","https://openalex.org/W2118238803","https://openalex.org/W2119504728","https://openalex.org/W2122680090","https://openalex.org/W2130410032","https://openalex.org/W2134988422","https://openalex.org/W2137864147","https://openalex.org/W2138207763","https://openalex.org/W2151702398","https://openalex.org/W2152325066","https://openalex.org/W2158945625","https://openalex.org/W2161817637","https://openalex.org/W2168108459","https://openalex.org/W2169456326","https://openalex.org/W2179438025","https://openalex.org/W2269247182","https://openalex.org/W2271989793","https://openalex.org/W2325391880","https://openalex.org/W2327065964","https://openalex.org/W2346327373","https://openalex.org/W2464082044","https://openalex.org/W2512372054","https://openalex.org/W2528347464","https://openalex.org/W2756240008","https://openalex.org/W2889540146","https://openalex.org/W2898598946","https://openalex.org/W2910111050","https://openalex.org/W3108430752","https://openalex.org/W4233978776"],"related_works":["https://openalex.org/W2046632683","https://openalex.org/W1533984495","https://openalex.org/W2528347464","https://openalex.org/W2070517005","https://openalex.org/W2564810440","https://openalex.org/W2618594612","https://openalex.org/W3178882185","https://openalex.org/W2332173011","https://openalex.org/W2039169182","https://openalex.org/W2603516078"],"abstract_inverted_index":{"Prostate":[0],"cancer":[1,13],"(PCa)":[2],"patients":[3],"undergoing":[4],"androgen":[5,17],"deprivation":[6],"therapy":[7],"almost":[8],"invariably":[9],"develop":[10],"castration-resistant":[11],"prostate":[12],"(CRPC).":[14],"Targeting":[15],"the":[16,88],"receptor":[18],"(AR)":[19],"Binding":[20],"Function-3":[21],"(BF3)":[22],"site":[23],"offers":[24],"a":[25,58,127,135,142],"promising":[26],"option":[27],"to":[28],"treat":[29],"CRPC.":[30],"However,":[31],"BF3":[32,61],"inhibitors":[33],"have":[34],"been":[35],"limited":[36],"by":[37],"poor":[38],"potency":[39],"or":[40],"inadequate":[41],"metabolic":[42],"stability.":[43],"Through":[44],"extensive":[45],"medicinal":[46],"chemistry,":[47],"molecular":[48],"modeling,":[49],"and":[50,77,93,113,130],"biochemistry,":[51],"we":[52,103],"identified":[53],"2-(5,6,7-trifluoro-1":[54],"H":[55],"-Indol-3-yl)-quinoline-5-carboxamide":[56],"(VPC-13789),":[57],"potent":[59],"AR":[60,84],"antagonist":[62,85],"with":[63,121,134],"markedly":[64],"improved":[65],"pharmacokinetic":[66],"properties.":[67],"We":[68],"demonstrate":[69],"that":[70,109,140],"VPC-13789":[71,125],"suppresses":[72],"AR-mediated":[73],"transcription,":[74],"chromatin":[75],"binding,":[76],"recruitment":[78],"of":[79,90,119,138],"coregulatory":[80],"proteins.":[81],"This":[82],"novel":[83,145],"selectively":[86],"reduces":[87],"growth":[89],"both":[91],"androgen-dependent":[92],"enzalutamide-resistant":[94],"PCa":[95],"cell":[96],"lines.":[97],"Having":[98],"demonstrated":[99],"in":[100,116],"vitro":[101],"efficacy,":[102],"developed":[104],"an":[105],"orally":[106,131],"bioavailable":[107,132],"prodrug":[108],"reduced":[110],"PSA":[111],"production":[112],"tumor":[114],"volume":[115],"animal":[117],"models":[118],"CRPC":[120,146],"no":[122],"observed":[123],"toxicity.":[124],"is":[126],"potent,":[128],"selective,":[129],"antiandrogen":[133],"distinct":[136],"mode":[137],"action":[139],"has":[141],"potential":[143],"as":[144],"therapeutics.":[147]},"counts_by_year":[{"year":2026,"cited_by_count":2},{"year":2025,"cited_by_count":3},{"year":2023,"cited_by_count":3},{"year":2022,"cited_by_count":5}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2021-10-25T00:00:00"}