Synthesis, biological evaluation, and structure–activity relationship study of novel cytotoxic aza-caffeic acid derivatives

H Zou, H Wu, X Zhang, Y Zhao, J Stöckigt, Y Lou…

Index: Zou, Hongbin; Wu, Hao; Zhang, Xiangnan; Zhao, Yu; Stoeckigt, Joachim; Lou, Yijia; Yu, Yongping Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 17 p. 6351 - 6359

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Citation Number: 14

Abstract

Three series of aza-caffeic acid derivatives with different linkers were designed and synthesized. Each of the synthesized derivatives was then used in cytotoxicity screening on either 8 or 12 human cancer cell lines. The structure–activity relationships on three structural regions A, B, and C are analyzed in detail, indicating that a nine bond linker B, containing a piperazine unit, is the most favorable linker leading to the generation of molecules with ...