Wu, Tian-bang; Xiang, Qiu-ping; Wang, Chao; Wu, Chun; Zhang, Cheng; Zhang, Mao-feng; Liu, Zhao-xuan; Zhang, Yan; Xiao, Lin-jiu; Xu, Yong published the artcile< Y06014 is a selective BET inhibitor for the treatment of prostate cancer>, Formula: C7H6Cl2O3S, the main research area is dimethylisoxazolyl benzoindolone preparation BET inhibitor SAR antitumor human docking; BRD4; Y06014; androgen receptor; bromodomain inhibitor; prostate cancer.
The design, synthesis and a structure-activity relationship study of 6-(3,5-dimethylisoxazol-4-yl)benzo[cd]indol-2(1H)-one derivative I [R = Et, PhSO2, PhCH2CH2CH2, etc.] as novel selective BET inhibitors was reported. One representative compound, compound I [R = Et], bound to BRD4(1) in the low micromolar range and demonstrated high selectivity for BRD4(1) over other non-BET bromodomain-containing proteins. This mol. also potently inhibited cell growth, colony formation and mRNA expression of AR-regulated genes in PC cell lines. The compound I [R = Et] also showed stronger activity than the second-generation antiandrogen enzalutamide. The compound I [R = Et] might serve as a new small mol. probe for further validation of BET as a mol. target for PC drug development.
Acta Pharmacologica Sinica published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Formula: C7H6Cl2O3S.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics