{"id":"https://openalex.org/W2516397751","doi":"https://doi.org/10.1111/cbdd.12812","title":"Synthesis, biological evaluation, and molecular docking studies of new pyrazol\u20103\u2010one derivatives with aromatase inhibition activities","display_name":"Synthesis, biological evaluation, and molecular docking studies of new pyrazol\u20103\u2010one derivatives with aromatase inhibition activities","publication_year":2016,"publication_date":"2016-08-27","ids":{"openalex":"https://openalex.org/W2516397751","doi":"https://doi.org/10.1111/cbdd.12812","mag":"2516397751","pmid":"https://pubmed.ncbi.nlm.nih.gov/27565954"},"language":"en","primary_location":{"id":"doi:10.1111/cbdd.12812","doi":"https://doi.org/10.1111/cbdd.12812","is_oa":false,"landing_page_url":"https://doi.org/10.1111/cbdd.12812","pdf_url":null,"source":{"id":"https://openalex.org/S123587420","display_name":"Chemical Biology & Drug Design","issn_l":"1747-0277","issn":["1747-0277","1747-0285"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-c","doyens","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Chemical Biology & Drug Design","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/A5023156490","display_name":"Xue\u2010Jing Yi","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4405253387","display_name":"Yueyang Vocational Technical College","ror":"https://ror.org/00kwqrp22","country_code":"CN","type":"education","lineage":["https://openalex.org/I4405253387"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Xue\u2010Jing Yi","raw_affiliation_strings":["Yueyang Vocational Technical College, Yueyang, China"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Yueyang Vocational Technical College, Yueyang, China","institution_ids":["https://openalex.org/I4405253387"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5072348811","display_name":"Tamer T. El\u2010Idreesy","orcid":"https://orcid.org/0000-0002-0170-9340","observed_orcids":["https://orcid.org/0000-0002-0170-9340"]},"institutions":[{"id":"https://openalex.org/I145487455","display_name":"Cairo University","ror":"https://ror.org/03q21mh05","country_code":"EG","type":"education","lineage":["https://openalex.org/I145487455"]},{"id":"https://openalex.org/I154023281","display_name":"British University in Egypt","ror":"https://ror.org/0066fxv63","country_code":"EG","type":"education","lineage":["https://openalex.org/I154023281"]}],"countries":["EG"],"is_corresponding":true,"raw_author_name":"Tamer T. El\u2010Idreesy","raw_affiliation_strings":["Department of Chemical Engineering, Faculty of Engineering, The British University in Egypt, El-Shorouk City, Egypt","Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemical Engineering, Faculty of Engineering, The British University in Egypt, El-Shorouk City, Egypt","institution_ids":["https://openalex.org/I154023281"]},{"raw_affiliation_string":"Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt","institution_ids":["https://openalex.org/I145487455"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5074710540","display_name":"Taha M. A. Eldebss","orcid":"https://orcid.org/0000-0002-1922-5037","observed_orcids":["https://orcid.org/0000-0002-1922-5037"]},"institutions":[{"id":"https://openalex.org/I145487455","display_name":"Cairo University","ror":"https://ror.org/03q21mh05","country_code":"EG","type":"education","lineage":["https://openalex.org/I145487455"]}],"countries":["EG"],"is_corresponding":true,"raw_author_name":"Taha M. A. Eldebss","raw_affiliation_strings":["Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt","institution_ids":["https://openalex.org/I145487455"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5073189555","display_name":"Ahmad M. Farag","orcid":"https://orcid.org/0000-0003-4796-1266","observed_orcids":["https://orcid.org/0000-0003-4796-1266"]},"institutions":[{"id":"https://openalex.org/I145487455","display_name":"Cairo University","ror":"https://ror.org/03q21mh05","country_code":"EG","type":"education","lineage":["https://openalex.org/I145487455"]}],"countries":["EG"],"is_corresponding":false,"raw_author_name":"Ahmad M. Farag","raw_affiliation_strings":["Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt","institution_ids":["https://openalex.org/I145487455"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5108106660","display_name":"Mohamed M. Abdulla","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Mohamed M. Abdulla","raw_affiliation_strings":["Research Unit, Saco Pharm. Co., 6th October City, Egypt"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Research Unit, Saco Pharm. Co., 6th October City, Egypt","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5046909486","display_name":"Shaimaa Hassan","orcid":"https://orcid.org/0000-0001-5635-9889","observed_orcids":["https://orcid.org/0000-0001-5635-9889"]},"institutions":[{"id":"https://openalex.org/I145487455","display_name":"Cairo University","ror":"https://ror.org/03q21mh05","country_code":"EG","type":"education","lineage":["https://openalex.org/I145487455"]}],"countries":["EG"],"is_corresponding":false,"raw_author_name":"Shaimaa A. Hassan","raw_affiliation_strings":["Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt","institution_ids":["https://openalex.org/I145487455"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5038486773","display_name":"Yahia N. Mabkhot","orcid":"https://orcid.org/0000-0002-9762-0323","observed_orcids":["https://orcid.org/0000-0002-9762-0323","https://orcid.org/0000-0002-2120-7567"]},"institutions":[{"id":"https://openalex.org/I28022161","display_name":"King Saud University","ror":"https://ror.org/02f81g417","country_code":"SA","type":"education","lineage":["https://openalex.org/I28022161"]}],"countries":["SA"],"is_corresponding":false,"raw_author_name":"Yahia N. Mabkhot","raw_affiliation_strings":["Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia","institution_ids":["https://openalex.org/I28022161"]}]}],"institutions":[],"countries_distinct_count":3,"institutions_distinct_count":4,"corresponding_author_ids":["https://openalex.org/A5072348811","https://openalex.org/A5074710540"],"corresponding_institution_ids":["https://openalex.org/I145487455","https://openalex.org/I154023281"],"apc_list":{"value":3920,"currency":"USD","value_usd":3920},"apc_paid":null,"fwci":0.9516,"has_fulltext":false,"cited_by_count":25,"citation_normalized_percentile":{"value":0.68916774,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":89,"max":98},"biblio":{"volume":"88","issue":"6","first_page":"832","last_page":"843"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.9907000064849854,"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"}},"topics":[{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.9907000064849854,"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/T10756","display_name":"Estrogen and related hormone effects","score":0.004999999888241291,"subfield":{"id":"https://openalex.org/subfields/1310","display_name":"Endocrinology"},"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/T14099","display_name":"Synthesis and Characterization of Heterocyclic Compounds","score":0.0010000000474974513,"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"}}],"keywords":[{"id":"https://openalex.org/keywords/aromatase-inhibition","display_name":"aromatase inhibition","score":0.9549999833106995},{"id":"https://openalex.org/keywords/letrozole","display_name":"letrozole","score":0.9559999704360962},{"id":"https://openalex.org/keywords/estrogen-synthesis-inhibition","display_name":"estrogen synthesis inhibition","score":0.5270000100135803},{"id":"https://openalex.org/keywords/molecular-docking","display_name":"molecular docking","score":0.656000018119812},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.6880000233650208},{"id":"https://openalex.org/keywords/anticancer-agents","display_name":"anticancer agents","score":0.47699999809265137}],"concepts":[{"id":"https://openalex.org/C2778812593","wikidata":"https://www.wikidata.org/wiki/Q194974","display_name":"Letrozole","level":5,"score":0.9235786199569702},{"id":"https://openalex.org/C2776166826","wikidata":"https://www.wikidata.org/wiki/Q415287","display_name":"Aromatase","level":4,"score":0.8712632656097412},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.6368186473846436},{"id":"https://openalex.org/C2777752497","wikidata":"https://www.wikidata.org/wiki/Q286779","display_name":"IC50","level":3,"score":0.6345773935317993},{"id":"https://openalex.org/C41685203","wikidata":"https://www.wikidata.org/wiki/Q1974042","display_name":"Docking (animal)","level":2,"score":0.5968795418739319},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.5799469351768494},{"id":"https://openalex.org/C2778504769","wikidata":"https://www.wikidata.org/wiki/Q3040305","display_name":"Aromatase inhibitor","level":5,"score":0.5432968139648438},{"id":"https://openalex.org/C2779715943","wikidata":"https://www.wikidata.org/wiki/Q427492","display_name":"Enzyme inhibition","level":3,"score":0.4732533097267151},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.45997926592826843},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.4018491804599762},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.39200764894485474},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.263005793094635},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.1841317117214203},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.16412290930747986},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.10343217849731445},{"id":"https://openalex.org/C54355233","wikidata":"https://www.wikidata.org/wiki/Q7162","display_name":"Genetics","level":1,"score":0.06982293725013733},{"id":"https://openalex.org/C121608353","wikidata":"https://www.wikidata.org/wiki/Q12078","display_name":"Cancer","level":2,"score":0.0},{"id":"https://openalex.org/C530470458","wikidata":"https://www.wikidata.org/wiki/Q128581","display_name":"Breast cancer","level":3,"score":0.0},{"id":"https://openalex.org/C159110408","wikidata":"https://www.wikidata.org/wiki/Q121176","display_name":"Nursing","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D013057","descriptor_name":"Spectrum Analysis","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":false},{"descriptor_ui":"D013816","descriptor_name":"Thermodynamics","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D020128","descriptor_name":"Inhibitory Concentration 50","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D047069","descriptor_name":"Pyrazolones","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D047069","descriptor_name":"Pyrazolones","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D047069","descriptor_name":"Pyrazolones","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D047072","descriptor_name":"Aromatase Inhibitors","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D047072","descriptor_name":"Aromatase Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D047072","descriptor_name":"Aromatase Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D062105","descriptor_name":"Molecular Docking Simulation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1111/cbdd.12812","doi":"https://doi.org/10.1111/cbdd.12812","is_oa":false,"landing_page_url":"https://doi.org/10.1111/cbdd.12812","pdf_url":null,"source":{"id":"https://openalex.org/S123587420","display_name":"Chemical Biology & Drug Design","issn_l":"1747-0277","issn":["1747-0277","1747-0285"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-c","doyens","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Chemical Biology & Drug Design","raw_type":"journal-article"},{"id":"pmid:27565954","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/27565954","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":"Chemical biology & drug design","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.6240000128746033}],"study_designs":[],"awards":[],"funders":[{"id":"https://openalex.org/F4320326607","display_name":"Universit\u00e0 degli Studi di Camerino","ror":"https://ror.org/0005w8d69"},{"id":"https://openalex.org/F4320335726","display_name":"Deanship of Scientific Research, King Saud University","ror":null}],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":27,"referenced_works":["https://openalex.org/W1572500512","https://openalex.org/W1598892184","https://openalex.org/W1973737572","https://openalex.org/W1977182996","https://openalex.org/W1977599555","https://openalex.org/W1978203969","https://openalex.org/W1982820526","https://openalex.org/W1984262137","https://openalex.org/W1984858425","https://openalex.org/W1991338244","https://openalex.org/W2008481614","https://openalex.org/W2019010482","https://openalex.org/W2028126678","https://openalex.org/W2028129845","https://openalex.org/W2028270669","https://openalex.org/W2031548407","https://openalex.org/W2041963383","https://openalex.org/W2054668663","https://openalex.org/W2063742494","https://openalex.org/W2084110162","https://openalex.org/W2109617076","https://openalex.org/W2144431312","https://openalex.org/W2168782278","https://openalex.org/W2343143290","https://openalex.org/W2949803452","https://openalex.org/W2950441455","https://openalex.org/W2951677317"],"related_works":["https://openalex.org/W1969183721","https://openalex.org/W2953294501","https://openalex.org/W2784309406","https://openalex.org/W3014585561","https://openalex.org/W7169596564","https://openalex.org/W7125809482","https://openalex.org/W4415830417","https://openalex.org/W4387827367","https://openalex.org/W1973737572","https://openalex.org/W3012261016"],"abstract_inverted_index":{"A":[0],"new":[1],"series":[2,33],"derived":[3],"from":[4],"4\u2010(2\u2010chloroacetyl)\u20101,2\u2010dihydro\u20101,5\u2010dimethyl\u20102\u2010phenyl\u20103H\u2010pyrazol\u20103\u2010one":[5],"was":[6,17,34],"synthesized,":[7],"characterized":[8],"and":[9,19,58,73],"its":[10],"pharmacological":[11],"activity":[12],"toward":[13],"aromatase":[14],"enzyme":[15],"inhibition":[16,62],"screened":[18],"compared":[20,44],"to":[21,45,65,85],"the":[22,32,87],"reference":[23],"native":[24],"ligand":[25],"letrozole.":[26],"The":[27],"most":[28],"active":[29],"compound":[30],"of":[31,39,49],"16,":[35],"showing":[36],"IC50":[37,48,68],"value":[38],"0.0023":[40],"\u00b1":[41,51,71,75],"0.0002":[42],"\u03bcm":[43],"letrozole":[46,66],"with":[47,67],"0.0028":[50],"0.0006":[52],"\u03bcm.":[53],"In":[54],"addition,":[55],"compounds":[56],"26":[57],"36":[59],"exhibit":[60],"good":[61],"activities":[63],"close":[64],"values":[69],"0.0033":[70],"0.0001":[72],"0.0032":[74],"0.0003":[76],"\u03bcm,":[77],"respectively.":[78],"Moreover,":[79],"molecular":[80],"docking":[81],"studies":[82],"were":[83],"conducted":[84],"support":[86],"findings.":[88]},"counts_by_year":[{"year":2026,"cited_by_count":3},{"year":2025,"cited_by_count":1},{"year":2024,"cited_by_count":7},{"year":2022,"cited_by_count":2},{"year":2021,"cited_by_count":5},{"year":2019,"cited_by_count":4},{"year":2018,"cited_by_count":3}],"updated_date":"2026-11-10T11:39:43.021295","created_date":"2016-09-16T00:00:00"}