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Evaluation of Di-Sansalvamide A Derivatives: Synthesis, Structure-Activity Relationship, and Mechanism of Action

  作者 ALEXANDER LESLIE D; SELLERS ROBERT P; DAVIS MELINDA R; ARDI VERONICA C; JOHNSON VICTORIA A; VASKO ROBERT C; MCALPINE SHELLI R  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2009年52-24;  页码  7927-7930  
  关联知识点  
 

[摘要]Described is the SAR of 18 di-sansalvamide A derivatives and the mechanism of action of the most potent compound. We show that this scaffold is a promising lead in the development of novel cancer therapeutics because it is cytotoxic at nanomolar potency, inhibits a well-established oncogenic target (Hsp90), and does not share structural motifs with current drugs on the market.

 
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