64580-41-2Relevant articles and documents
2,3-diketone indole compound, preparation method and applications thereof
-
Paragraph 0149-0153, (2020/02/10)
The invention discloses a 2,3-diketone indole compound, a preparation method and applications thereof, wherein the compound has a structure represented by the following general formula (I) or (II). The invention further relates to a pharmaceutical composi
Discovery of novel 5-methyl-1H-pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation
Zhang, Daoguang,Asnake, Solomon,Zhang, Jingya,Olsson, Per-Erik,Zhao, Guisen
, p. 1113 - 1124 (2018/03/05)
Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective therapeutic target even for castration-resistant prostate cancer (CRPC). Herein, structural modification via a fragments splicing strategy was performed based on two lead compounds T3 and 10e, leading to the discovery of a series of 5-methyl-1H-pyrazole derivatives. AR reporter gene assay revealed compounds A13 and A14 as potent AR antagonists. Some of the compounds in this series inhibited growth of PCa LNCaP cells more efficiently than enzalutamide. A13 and A14 also showed improved metabolic stability compared with 10e in human liver microsomes.