Simplified aminocoumarin analogues as anticancer agents: Amino isosteric replacement in the noviose moiety resulted in substantial enhancement of antiproliferative activity |
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作者姓名: | Ting Zhang Zheng Yan Yun-Feng Li Nan Wang |
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作者单位: | State Key Laboratory of Bioactive Substance and Function of Natural Medicine,Beijing Key Laboratory of Active Substance Discovery and Drugability Evaluation,Institute of Materia Medico,Peking Union Medical College & Chinese Academy of Medical Sciences |
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基金项目: | support from Youth Science Foundation of Peking Union Medical College & Chinese Academy of Medical Sciences(No.521164) |
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摘 要: | Simplified aminocoumarin analogues,either noviosylated or simple basic heterocycle attached 3-amido-coumarin compounds,are known to be promising anticancer agents targeting the C-terminal ATP-binding site of Hsp90.In this study,3’-amino isosteric replacement in the noviose moiety of two known noviose containing Hsp90 C-terminal inhibitors was synthetically realized for the first time.In vitro evaluation of these compounds suggested that the introduction of a basic amino group into the noviose subunit resulted in significant improvement of their cytotoxicities.
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关 键 词: | 3-Amino-3-deoxy-L-noviose Aminocoumarin analogues Cytotoxicity Hsp90 inhibitors |
收稿时间: | 2013-03-05 |
修稿时间: | 2013-04-18 |
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