1612893-77-2Relevant academic research and scientific papers
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.
