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 ...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.展开更多
基金support from Youth Science Foundation of Peking Union Medical College & Chinese Academy of Medical Sciences(No.521164)
文摘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.
