{"id":"https://openalex.org/W560142897","doi":null,"title":"Cytotoxic thiol alkylators containing the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore","display_name":"Cytotoxic thiol alkylators containing the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore","publication_year":2012,"publication_date":"2012-07-01","ids":{"openalex":"https://openalex.org/W560142897","mag":"560142897"},"language":"en","primary_location":{"id":"pmh:oai:harvest.usask.ca:10388/ETD-2012-07-543","doi":null,"is_oa":true,"landing_page_url":"https://hdl.handle.net/10388/ETD-2012-07-543","pdf_url":"https://harvest.usask.ca/bitstreams/e1ff1291-8512-4d4d-ac80-4458adc00eb0/download","source":{"id":"https://openalex.org/S7407063267","display_name":"HARVEST (University of Saskatchewan)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":"Thesis"},"volume":null,"type":"dissertation","is_traditional":true,"indexed_in":[],"open_access":{"is_oa":true,"oa_status":"green","oa_url":"https://harvest.usask.ca/bitstreams/e1ff1291-8512-4d4d-ac80-4458adc00eb0/download","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5100829904","display_name":"Swagatika Das","orcid":"https://orcid.org/0000-0002-2721-5664","observed_orcids":["https://orcid.org/0000-0002-2721-5664"]},"institutions":[],"countries":[],"is_corresponding":true,"raw_author_name":"Swagatika Das","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":["https://openalex.org/A5100829904"],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":true,"cited_by_count":0,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11319","display_name":"Curcumin's Biomedical Applications","score":0.6718999743461609,"subfield":{"id":"https://openalex.org/subfields/1313","display_name":"Molecular Medicine"},"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/T11319","display_name":"Curcumin's Biomedical Applications","score":0.6718999743461609,"subfield":{"id":"https://openalex.org/subfields/1313","display_name":"Molecular Medicine"},"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":0.29739999771118164,"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/T12189","display_name":"Sulfur-Based Synthesis Techniques","score":0.0017999999690800905,"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/curcuminoids","display_name":"curcuminoids","score":0.8759999871253967},{"id":"https://openalex.org/keywords/cytotoxicity","display_name":"cytotoxicity","score":0.6819999814033508},{"id":"https://openalex.org/keywords/anticancer-drug-design","display_name":"anticancer drug design","score":0.6769999861717224},{"id":"https://openalex.org/keywords/multidrug-resistance","display_name":"multidrug resistance","score":0.7789999842643738},{"id":"https://openalex.org/keywords/selective-toxicity","display_name":"selective toxicity","score":0.3529999852180481},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.5049999952316284}],"concepts":[{"id":"https://openalex.org/C56173144","wikidata":"https://www.wikidata.org/wiki/Q1539893","display_name":"Pharmacophore","level":2,"score":0.8516929149627686},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.6877102851867676},{"id":"https://openalex.org/C2781324293","wikidata":"https://www.wikidata.org/wiki/Q220410","display_name":"Thiol","level":2,"score":0.6785961389541626},{"id":"https://openalex.org/C154317977","wikidata":"https://www.wikidata.org/wiki/Q376266","display_name":"Cytotoxic T cell","level":3,"score":0.5304859280586243},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.43875396251678467},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3582763075828552},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.07344073057174683}],"mesh":[],"locations_count":3,"locations":[{"id":"pmh:oai:harvest.usask.ca:10388/ETD-2012-07-543","doi":null,"is_oa":true,"landing_page_url":"https://hdl.handle.net/10388/ETD-2012-07-543","pdf_url":"https://harvest.usask.ca/bitstreams/e1ff1291-8512-4d4d-ac80-4458adc00eb0/download","source":{"id":"https://openalex.org/S7407063267","display_name":"HARVEST (University of Saskatchewan)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":"Thesis"},{"id":"pmh:oai:ecommons.usask.ca:10388/ETD-2012-07-543","doi":null,"is_oa":false,"landing_page_url":"http://hdl.handle.net/10388/ETD-2012-07-543","pdf_url":null,"source":{"id":"https://openalex.org/S4377196608","display_name":"University Library - University of Saskatchewan (University of Saskatchewan)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I32625721","host_organization_name":"University of Saskatchewan","host_organization_lineage":["https://openalex.org/I32625721"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"","raw_type":"thesis"},{"id":"mag:560142897","doi":null,"is_oa":false,"landing_page_url":"https://harvest.usask.ca/bitstream/10388/ETD-2012-07-543/4/DAS-DISSERTATION.pdf","pdf_url":null,"source":null,"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":null}],"best_oa_location":{"id":"pmh:oai:harvest.usask.ca:10388/ETD-2012-07-543","doi":null,"is_oa":true,"landing_page_url":"https://hdl.handle.net/10388/ETD-2012-07-543","pdf_url":"https://harvest.usask.ca/bitstreams/e1ff1291-8512-4d4d-ac80-4458adc00eb0/download","source":{"id":"https://openalex.org/S7407063267","display_name":"HARVEST (University of Saskatchewan)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":"Thesis"},"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.8371999859809875}],"study_designs":[],"awards":[],"funders":[{"id":"https://openalex.org/F4320319919","display_name":"Saskatchewan Health Research Foundation","ror":"https://ror.org/00trnds81"},{"id":"https://openalex.org/F4320327336","display_name":"Vlaamse regering","ror":null},{"id":"https://openalex.org/F4320333121","display_name":"University of Texas at El Paso","ror":"https://ror.org/04d5vba33"},{"id":"https://openalex.org/F4320334506","display_name":"Canadian Institutes of Health Research","ror":"https://ror.org/01gavpb45"},{"id":"https://openalex.org/F4320337351","display_name":"National Cancer Institute","ror":"https://ror.org/040gcmg81"}],"has_content":{"pdf":true,"grobid_xml":true},"content_urls":{"pdf":"https://content.openalex.org/works/W560142897.pdf","grobid_xml":"https://content.openalex.org/works/W560142897.grobid-xml"},"referenced_works_count":164,"referenced_works":["https://openalex.org/W44566723","https://openalex.org/W66356296","https://openalex.org/W132394059","https://openalex.org/W166752369","https://openalex.org/W296450459","https://openalex.org/W620000789","https://openalex.org/W982953202","https://openalex.org/W992836242","https://openalex.org/W1041184324","https://openalex.org/W1491596018","https://openalex.org/W1499700118","https://openalex.org/W1506756493","https://openalex.org/W1518635146","https://openalex.org/W1523213544","https://openalex.org/W1548122599","https://openalex.org/W1571190264","https://openalex.org/W1586129343","https://openalex.org/W1596848781","https://openalex.org/W1609919210","https://openalex.org/W1632612050","https://openalex.org/W1828339576","https://openalex.org/W1871570718","https://openalex.org/W1915172695","https://openalex.org/W1964369488","https://openalex.org/W1965605561","https://openalex.org/W1966351884","https://openalex.org/W1967764146","https://openalex.org/W1967904223","https://openalex.org/W1968860225","https://openalex.org/W1969328947","https://openalex.org/W1969779044","https://openalex.org/W1970500885","https://openalex.org/W1971566724","https://openalex.org/W1976110644","https://openalex.org/W1977213462","https://openalex.org/W1978139448","https://openalex.org/W1979269391","https://openalex.org/W1979565006","https://openalex.org/W1981103392","https://openalex.org/W1982271708","https://openalex.org/W1984512827","https://openalex.org/W1985271353","https://openalex.org/W1986125636","https://openalex.org/W1988103584","https://openalex.org/W1988401864","https://openalex.org/W1990185112","https://openalex.org/W1990427439","https://openalex.org/W1994459746","https://openalex.org/W1996876030","https://openalex.org/W1996907401","https://openalex.org/W1997401961","https://openalex.org/W2000307014","https://openalex.org/W2002036002","https://openalex.org/W2004827880","https://openalex.org/W2011499737","https://openalex.org/W2012063336","https://openalex.org/W2012288058","https://openalex.org/W2012516837","https://openalex.org/W2013779256","https://openalex.org/W2014442719","https://openalex.org/W2015619170","https://openalex.org/W2019241564","https://openalex.org/W2020834684","https://openalex.org/W2021137848","https://openalex.org/W2022961049","https://openalex.org/W2023130049","https://openalex.org/W2023793608","https://openalex.org/W2026334721","https://openalex.org/W2027686496","https://openalex.org/W2028556682","https://openalex.org/W2030539713","https://openalex.org/W2030635414","https://openalex.org/W2030747159","https://openalex.org/W2031823798","https://openalex.org/W2032347891","https://openalex.org/W2033431239","https://openalex.org/W2035796149","https://openalex.org/W2039965018","https://openalex.org/W2041610556","https://openalex.org/W2043256069","https://openalex.org/W2043892945","https://openalex.org/W2044442595","https://openalex.org/W2044657300","https://openalex.org/W2044839967","https://openalex.org/W2045247659","https://openalex.org/W2045342567","https://openalex.org/W2047195231","https://openalex.org/W2048651813","https://openalex.org/W2048829869","https://openalex.org/W2053090763","https://openalex.org/W2054448934","https://openalex.org/W2057009086","https://openalex.org/W2057173428","https://openalex.org/W2057858743","https://openalex.org/W2058046287","https://openalex.org/W2058421614","https://openalex.org/W2063385957","https://openalex.org/W2063593425","https://openalex.org/W2064676317","https://openalex.org/W2064769568","https://openalex.org/W2067653691","https://openalex.org/W2070617886","https://openalex.org/W2071831214","https://openalex.org/W2072175441","https://openalex.org/W2074331690","https://openalex.org/W2074400320","https://openalex.org/W2075130174","https://openalex.org/W2077365696","https://openalex.org/W2079499545","https://openalex.org/W2079967197","https://openalex.org/W2080951960","https://openalex.org/W2081876939","https://openalex.org/W2090225356","https://openalex.org/W2090749980","https://openalex.org/W2092032160","https://openalex.org/W2094768851","https://openalex.org/W2095324891","https://openalex.org/W2097149924","https://openalex.org/W2097700251","https://openalex.org/W2098426299","https://openalex.org/W2099877688","https://openalex.org/W2104526249","https://openalex.org/W2106265598","https://openalex.org/W2114579003","https://openalex.org/W2124116148","https://openalex.org/W2125013139","https://openalex.org/W2135072453","https://openalex.org/W2135279270","https://openalex.org/W2137110320","https://openalex.org/W2139353173","https://openalex.org/W2140704233","https://openalex.org/W2141261575","https://openalex.org/W2145694409","https://openalex.org/W2145887093","https://openalex.org/W2147286656","https://openalex.org/W2149585271","https://openalex.org/W2150625778","https://openalex.org/W2151881294","https://openalex.org/W2152643523","https://openalex.org/W2159875179","https://openalex.org/W2161925427","https://openalex.org/W2163581938","https://openalex.org/W2164735889","https://openalex.org/W2165884308","https://openalex.org/W2166761147","https://openalex.org/W2167141095","https://openalex.org/W2167882141","https://openalex.org/W2168499664","https://openalex.org/W2171154502","https://openalex.org/W2173064381","https://openalex.org/W2179485306","https://openalex.org/W2317569972","https://openalex.org/W2328336008","https://openalex.org/W2346500611","https://openalex.org/W2409152330","https://openalex.org/W2409683568","https://openalex.org/W2415883663","https://openalex.org/W2493453162","https://openalex.org/W2792455800","https://openalex.org/W2951864513","https://openalex.org/W2955504961","https://openalex.org/W3133924569","https://openalex.org/W4292199267","https://openalex.org/W4313347802"],"related_works":["https://openalex.org/W140321345","https://openalex.org/W2916940911","https://openalex.org/W3149943529","https://openalex.org/W2015619170","https://openalex.org/W2150625778","https://openalex.org/W2960291595","https://openalex.org/W3042828624","https://openalex.org/W3161231892","https://openalex.org/W2998751838","https://openalex.org/W2057009086"],"abstract_inverted_index":{"For":[0],"the":[1,83,90,100,110,113,152,159,209,216,224,242,249,256,282,333,338,342,345,350,354,376,380,390,394,399,432,452,459,476,483,562,581,671,710,713],"last":[2],"several":[3],"years":[4],"curcumin":[5,84],"has":[6,87,180,461],"attracted":[7],"considerable":[8],"interest":[9],"due":[10],"to":[11,14,44,81,89,109,120,140,148,158,175,183,187,197,260,273,278,327,368,374,425,468,471,513,523,530,540,613,667,720],"its":[12,42,54,65],"ability":[13,147,169,535],"inhibit":[15],"cancer":[16,37,316,480],"cell":[17,30,559,578,652],"proliferation":[18],"in":[19,22,36,165,204,315,341,398,458,479,497,552,556,575,621,691],"vitro":[20],"and":[21,32,60,124,161,417,420,438,465,502,519,580,614,623,651,666,688],"vivo":[23],"by":[24,78,103,194,305,382,486,528],"targeting":[25],"a":[26,48,68,104,289,306,412,444,489,546,557,576,593,609,633,660,674],"number":[27,453,490,566,634,675],"of":[28,92,99,112,131,155,170,173,211,226,244,255,284,291,332,337,353,379,393,404,415,431,454,475,491,517,536,549,567,601,603,630,632,635,673,676,698,709,712],"different":[29,515],"signaling":[31],"molecular":[33],"mechanism":[34],"pathways":[35,179],"cells.":[38,275,320,429,473],"These":[39],"results":[40],"prove":[41],"potential":[43,661],"be":[45,121,184,234,521,590],"considered":[46,182],"as":[47,67,141,219,236,387,592,659],"future":[49,696],"anticancer":[50,199,237,447,507,532,664],"drug":[51,70,238,525,544,550],"candidate.":[52,71],"However":[53],"metabolic":[55],"instability,":[56],"low":[57],"oral":[58],"bioavailability":[59],"high":[61,126],"clearance":[62],"have":[63,75,371],"limited":[64],"use":[66],"clinical":[69],"Subsequently":[72],"enormous":[73],"efforts":[74],"been":[76,181,372],"expended":[77],"medicinal":[79],"chemists":[80],"modify":[82],"structure":[85],"which":[86,117,133,231,264,294,363,642],"led":[88,108],"development":[91,210,697],"novel":[93,212,245,262,395,537],"cytotoxic":[94,127,221,409,423,436,463,538,638],"curcuminoid":[95,213],"analogs.":[96],"The":[97,168,321,494,534,628,655,684],"replacement":[98],"\u03b2-diketone":[101],"moiety":[102],"mono":[105],"carbonyl":[106],"group":[107,716],"discovery":[111],"1,5-diaryl-3-oxo-1,4-":[114],"pentadienyl":[115],"pharmacophore":[116,218,340],"was":[118,259,286,325,554,682],"found":[119],"metabolically":[122],"stable":[123],"demonstrate":[125,569],"potencies.":[128],"This":[129],"class":[130,172],"compounds":[132,174,406,685],"possesses":[134],"multiple":[135,177],"alkylating":[136,446,456],"sites":[137,457],"are":[138,500,511,701],"referred":[139],"thiol":[142,153,455],"alkylators":[143],"based":[144,247,287],"on":[145,208,248,288,301,330,679],"their":[146],"interact":[149,357],"preferentially":[150],"with":[151,223,561],"groups":[154,163,385],"macromolecules":[156],"compared":[157,272,470],"hydroxy":[160],"amino":[162],"present":[164],"nucleic":[166],"acids.":[167],"this":[171,205,498,669,707,723],"target":[176,662],"biochemical":[178],"an":[185,297,359],"advantage":[186],"overcome":[188,524],"multidrug":[189,571,595],"resistance":[190,484,526,551,572,596],"that":[191,296,402,584,607,706],"is":[192,252,482,583,606,618,657,704],"shown":[193,485,527],"many":[195,403,602],"tumours":[196,469,529],"current":[198,202],"drugs.":[200],"My":[201],"work":[203],"report":[206,499],"focuses":[207],"analogs":[214],"possessing":[215],"1,5-diaryl-3-oxo-1,4-pentadienyl":[217,339],"potent":[220,408,594,637,677],"agents":[222,539,665],"aspiration":[225,582],"identifying":[227],"some":[228],"lead":[229],"molecules":[230,285,343,381,396,433,495,568,588,639,700],"can":[232,589],"further":[233],"developed":[235,591],"candidates.":[239],"In":[240,276,449],"particular,":[241],"synthesis":[243],"curcuminoids":[246,605],"3,5-bis(arylidene)-4-piperidone":[250],"nucleus":[251],"pursued.":[253],"One":[254,474],"main":[257],"objectives":[258],"produce":[261],"cytotoxins":[263,678],"will":[265,310,717],"display":[266,407,514],"selective":[267,466],"toxicity":[268,367],"towards":[269,411,488],"malignant":[270],"cells":[271,317,419],"normal":[274,319,428,472],"order":[277],"obtain":[279],"tumour-selective":[280],"cytotoxins,":[281],"design":[283],"theory":[290],"sequential":[292,322],"cytotoxicity":[293],"states":[295],"initial":[298],"chemical":[299,308],"attack":[300,309],"cellular":[302],"constituents":[303],"followed":[304],"second":[307],"cause":[311],"more":[312,587],"damaging":[313],"effects":[314],"than":[318,427,442],"alkylation":[323],"reaction":[324],"proposed":[326],"take":[328],"place":[329],"both":[331],"olefinic":[334],"carbon":[335],"atoms":[336],"at":[344,358],"primary":[346],"binding":[347,361],"site":[348,362],"whereas":[349],"other":[351],"part":[352],"molecule":[355,460],"would":[356],"auxiliary":[360],"may":[364,520],"confer":[365],"preferential":[366],"tumours.":[369],"Efforts":[370],"made":[373],"improve":[375],"physicochemical":[377],"properties":[378,410,574],"introducing":[383],"hydrophilic":[384],"such":[386],"phosphates":[388],"onto":[389],"molecules.":[391],"Bioevaluations":[392],"disclosed":[397],"thesis":[400],"revealed":[401],"these":[405,604,699],"wide":[413],"range":[414],"neoplastic":[416,558,577],"transformed":[418],"show":[421],"greater":[422,439],"potencies":[424,437,464],"neoplasms":[426],"Most":[430],"demonstrated":[434],"higher":[435],"tumour":[440],"selectivity":[441],"melphalan,":[443],"reference":[445],"drug.":[448],"general,":[450],"increasing":[451],"increased":[462],"toxicities":[467],"major":[477,547],"challenges":[478],"treatment":[481],"tumors":[487],"chemotherapeutic":[492],"agents.":[493,533],"designed":[496],"chemically":[501],"structurally":[503],"divergent":[504],"from":[505],"established":[506],"drugs;":[508],"therefore":[509],"they":[510],"expected":[512],"modes":[516,629],"action":[518,631],"able":[522],"contemporary":[531],"modulate":[541],"P-glycoprotein":[542],"mediated":[543],"resistance,":[545],"form":[548],"cancers,":[553],"verified":[555],"transfected":[560],"mdr1":[563],"gene.":[564],"A":[565,598],"remarkable":[570],"reversal":[573],"line":[579],"one":[585],"or":[586],"modulator.":[597],"striking":[599],"feature":[600],"using":[608],"dose":[610],"level":[611],"up":[612],"including":[615],"300":[616],"mg/kg":[617],"well":[619],"tolerated":[620],"mice":[622],"displays":[624],"no":[625],"significant":[626],"toxicities.":[627],"representative":[636],"were":[640],"evaluated":[641],"include":[643],"apoptosis,":[644],"caspase-3":[645],"activation,":[646],"DNA":[647],"fragmentation,":[648],"PARP":[649],"cleavage":[650],"cycle":[653],"arrest.":[654],"mitochondrion":[656],"emerging":[658],"for":[663,695],"evaluate":[668],"possibility,":[670],"effect":[672],"mitochondrial":[680],"functions":[681],"verified.":[683],"affected":[686],"respiration":[687],"caused":[689],"swelling":[690],"mitochondria.":[692],"Some":[693],"guidelines":[694],"suggested.":[702],"It":[703],"hoped":[705],"eulogy":[708],"importance":[711],"conjugated":[714],"dienone":[715],"encourage":[718],"researchers":[719],"consider":[721],"incorporating":[722],"structural":[724],"unit":[725],"into":[726],"candidate":[727],"cytotoxins.":[728]},"counts_by_year":[],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}
