title: Discovery of 1H-indole-2-carboxamides as novel inhibitors of the androgen receptor binding function 3 (BF3).
abstract: To overcome resistance to conventional anti-androgens of human androgen receptor (AR), the allosteric site of the AR binding function 3 (BF3) was investigated as an alternative target for small molecule therapeutics. A library of 1H-indole-2-carboxamides were discovered as BF3 inhibitors and exhibited strong antiproliferative activity against LNCaP and enzalutamide-resistant prostate cancer cell lines. Several of the lead compounds may prove of particular benefit as a novel alternative treatment for castration-resistant prostate cancers.
authors.affiliation: Vancouver Prostate Centre, University of British Columbia , 2660 Oak Street, Vancouver, British Columbia V6H 3Z6, Canada.
authors.forename: Fuqiang
authors.initials: F
authors.lastname: Ban
authors.forename: Eric
authors.initials: E
authors.lastname: Leblanc
authors.forename: Huifang
authors.initials: H
authors.lastname: Li
authors.forename: Ravi S N
authors.initials: RS
authors.lastname: Munuganti
authors.forename: Kate
authors.initials: K
authors.lastname: Frewin
authors.forename: Paul S
authors.initials: PS
authors.lastname: Rennie
authors.forename: Artem
authors.initials: A
authors.lastname: Cherkasov
mesh_terms: D000495:Allosteric Site; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D008958:Models, Molecular; D064129:Prostatic Neoplasms, Castration-Resistant / Q000188:drug therapy; D011944:Receptors, Androgen / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D007211:Indoles; D011944:Receptors, Androgen; D054852:Small Molecule Libraries