Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase

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• 作者：Gurulingappa ; Hallur ; Buckhalts ; Phillip ; Kinzler ; Kenneth W. ; Vogelstein ; Bert ; Khan ; Saeed R.
• 关键词：Aminophosphinic acid derivatives ; RDP inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2004
• 出版时间：July 5, 2004
• 年：2004
• 卷：14
• 期：13
• 页码：3531-3533
• 全文大小：248 K

文摘

Renal dipeptidase (RDP) is an enzyme overexpressed in benign and malignant colorectal tumors. In an effort to identify potent inhibitors of this enzyme, a series of aminophosphinic acid derivatives were synthesized. Compounds 3a and 3c in which the phenyl ring was para substituted with F and Br and olefin with Z geometry, showed better inhibitory activity against RDP enzyme (IC₅₀