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

Abstract

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.