Semi-synthetic aristolactams—inhibitors of CDK2 enzyme

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• 作者：Vinod R. Hegde ; Scott Borges ; Haiyan Pu ; Mahesh Patel ; Vincent P. Gullo ; Bonnie Wu ; Paul Kirschmeier ; Michael J. Williams ; Vincent Madison ; Thierry Fischmann ; Tze-Ming Chan
• 关键词：Semi-synthetic analogs ; Aristolactams ; IC₅₀ ; SAR
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 February 2010
• 年：2010
• 卷：20
• 期：4
• 页码：1384-1387
• 全文大小：321 K

文摘

Several analogs of aristolochic acids were isolated and derivatized into their lactam derivatives to study their inhibition in CDK2 assay. The study helped to derive some conclusions about the structure–activity relation around the phenanthrin moiety. Semi-synthetic aristolactam 21 showed good activity with inhibition IC₅₀ of 35 nM in CDK2 assay. The activity of this compound was comparable to some of the most potent synthetic compounds reported in the literature.