158089-10-2Relevant academic research and scientific papers
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.
Cyclohex-1-ene carboxylic acids: Synthesis and biological evaluation of novel inhibitors of human 5α reductase
Baston, Eckhard,Salem, Ola I. A.,Hartmann, Rolf W.
, p. 31 - 38 (2007/10/03)
In search of novel nonsteroidal mimics of steroidal inhibitors of 5α reductase, 4-(2-phenylethyl)cyclohex-1-ene carboxylic acids 1-5 were synthesized with different substituents in para position of the phenyl ring (1: N,N-diisopropylcarbamoyl, 2: phenyl,
Novel 5α-reductase inhibitors. Synthesis and structure-activity studies of 5-substituted 1-methyl-2-pyridones and 1-methyl-2-piperidones
Hartmann, R. W.,Reichert, M.,Goehring, S.
, p. 807 - 818 (2007/10/02)
In search for nonsteroidal inhibitors of 5α-reductase for the treatment of benign prostatic hyperplasia (BPH) and possibly prostate cancer, substrate mimicks were synthesized comprising of a 1-methyl-2-pyridone (2, 4-16) or 1-methyl-2-piperidone (1, 3, 17
