Synthesis and structure–activity relationships of N-aryl (indol-3-yl) glyoxamides as antitumor agents

P Marchand, M Antoine, G Le Baut, M Czech…

Index: Marchand, Pascal; Antoine, Maud; Baut, Guillaume Le; Czech, Michael; Baasner, Silke; Guenther, Eckhard Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 18 p. 6715 - 6727

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Citation Number: 13

Abstract

The synthesis and study of the structure–activity relationships of cytotoxic compounds based on N-pyridinyl or N-aryl-2-(1-benzylindol-3-yl) glyoxamide skeleton, represented by the lead structures D-24241 and D-24851, are described. The presence of N-(pyridin-4-yl) moiety was crucial for activity and 2-[1-(4-chloro-3-nitrobenzyl)-1H-indol-3-yl]-2-oxo-N-(pyridin-4-yl) acetamide (55), the most potent derivative, showed IC50= 39nM, 51nM and 11nM against ...