Citation: Jun Hang Jiang, Xue Fei Liu, Can Hui Zhen, You Jun Zhou, Ju Zhu, Jia Guo Lv, Chun Quan Sheng. Acrosin structure-based design, synthesis and biological activities of 7-azaindol derivatives as new acrosin inhibitors[J]. Chinese Chemical Letters, ;2011, 22(3): 272-275. doi: 10.1016/j.cclet.2010.09.033 shu

Acrosin structure-based design, synthesis and biological activities of 7-azaindol derivatives as new acrosin inhibitors

Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 8 June 2010

Fund Project: This work was supported by the Shanghai Family Planning Commission Research Fund (No. 2007JG02) and Shanghai Leading Academic Discipline Project (No. B906).

A series of 7-azaindol derivatives were designed based on the homologous 3D model of human acrosin. These compounds were synthesized and evaluated for their human acrosin inhibitory activities in vitro. Compounds 7a, 7i, 7j, 7k and 7n showed highly inhibitory activity against human acrosin. The three-dimensional structure-activity relationship was investigated through a CoMFA model, which provided valuable information to further study of potential human acrosin inhibitors.
- Rational design,
- Azaindole,
- Synthesis,
- Acrosin,
- CoMFA
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