In 2022,Xiang, Qiuping; Wang, Chao; Wu, Tianbang; Zhang, Cheng; Hu, Qingqing; Luo, Guolong; Hu, Jiankang; Zhuang, Xiaoxi; Zou, Lingjiao; Shen, Hui; Wu, Xishan; Zhang, Yan; Kong, Xiangqian; Liu, Jinsong; Xu, Yong published an article in Journal of Medicinal Chemistry. The title of the article was 《Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer》.SDS of cas: 329-59-9 The author mentioned the following in the article:
Herein, the structural optimization of a series of 1-(indolizin-3-yl)ethan-1-one compounds I (R1 = Me, Et, NHMe, i-Pr, t-Bu, cyclopropyl; R2 = Me, Et, MeO, OH, NH2, PhCH2O, t-BuCO2, etc.; R3 = F, Cl, CH2OH, etc.; R4 = Me, cyclopropyl) as new selective CBP bromodomain inhibitors, aiming to improve cellular potency and metabolic stability, is reported. This process led to the compound I [R1 = Me; R2 = MeO; R3 = CH(OH)Me; R4 = cyclopropyl], which possesses good liver microsomal stability and pharmacokinetic properties (F = 25.9%). Furthermore, this compound is able to inhibit CBP bromodomain as well as the proliferation, colony formation, and migration of prostate cancer cells. Addnl., the new inhibitor shows promising antitumor efficacy in a 22Rv1 xenograft model (TGI = 88%). This study provides new lead compounds for further development of drugs for the treatment of prostate cancer. The experimental process involved the reaction of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9SDS of cas: 329-59-9)
Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.SDS of cas: 329-59-9
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics