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Weiwei Ning, Ju Zhu, Canhui Zheng, Xuefei Liu, Yunlong Song, Youjun Zhou, Xiaomeng Zhang, Ling Zhang, Chunquan Sheng and Jiaguo Lv Fragment-Based Design of Novel Quinazolinon Derivatives as Human Acrosin Inhibitors Chemical Biology & Drug Design 81

Article first published online: 28 MAR 2013 | DOI: 10.1111/cbdd.12106

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On the basis of the active site of human acrosin, a series of novel quinazolinon derivatives were designed and synthesized by a fragment docking and growing strategy. Compound 5g showed potent human acrosin inhibitory activity and was more active than the known inhibitors.

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