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

作者：Jiang Jun Hang; Liu Xue Fei; Zhen Can Hui; Zhou You Jun; Zhu Ju; Lv Jia Guo^*; Sheng Chun Quan

来源：Chinese Chemical Letters, 2011, 22(3): 272-275.

DOI：10.1016/j.cclet.2010.09.033

• Rational design
• Azaindole
• Synthesis
• Acrosin
• CoMFA

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.

• 出版日期2011-3
• 单位中国人民解放军第二军医大学