1369430-38-5Relevant articles and documents
Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors
Zhao, Juntao,Tian, Wei,Qi, Jingjing,Lv, Diya,Liu, Yang,Jiang, Yan,Dong, Guoqiang,Chen, Qianqian,Zhou, Youjun,Zhu, Ju,Wang, Heling,Sheng, Chunquan,Lv, Jiaguo
, p. 2802 - 2806 (2014/06/10)
Human acrosin is an attractive target for the discovery of novel male contraceptives. Isoxazole derivative ISO-1, a small-molecule weak human acrosin inhibitor, was used as the starting point for lead optimization. After two rounds of structure-based inhibitor design, a highly potent inhibitor B6 (IC50 = 1.44 μM) was successfully identified, which showed good selectivity over trypsin and represents one of the most active human acrosin inhibitors up to date.