Simplified aminocoumarin analogues as anticancer agents：Amino isosteric replacement in the noviose moiety resulted in substantial enhancement of antiproliferative activity

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 novios...

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Bibliographic Details
Published in:Chinese chemical letters 2013-08, Vol.24 (8), p.719-722
Main Authors: Zhang, Ting, Yan, Zheng, Li, Yun-Feng, Wang, Nan
Format: Article
Language:English
Subjects:
3-Amino-3-deoxy-l-noviose
Aminocoumarin analogues
Cytotoxicity
Hsp90
Hsp90 inhibitors
增殖活性
抗癌药物
热休克蛋白90
类似物
置换
酰氨基
香豆素类化合物
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Summary: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.
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2013.04.046