Citation: Ting Zhang, Zheng Yan, Yun-Feng Li, Nan Wang. Simplified aminocoumarin analogues as anticancer agents: Amino isosteric replacement in the noviose moiety resulted in substantial enhancement of antiproliferative activity[J]. Chinese Chemical Letters, ;2013, 24(8): 719-722. shu

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

  • Corresponding author: Yun-Feng Li,  Nan Wang, 
  • Received Date: 5 March 2013
    Available Online: 18 April 2013

  • Simplified aminocoumarin analogues, either noviosylated or simple basic heterocycle attached 3-amidocoumarin compounds, are known to be promising anticancer agents targeting the C-terminal ATPbinding 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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