Evaluation of Di-Sansalvamide A Derivatives: Synthesis, Structure−Activity Relationship, and Mechanism of Action
Journal of Medicinal Chemistry2009Vol. 52(24), pp. 7927–7930
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Leslie D. Alexander, Robert P. Sellers, Melinda R. Davis, Veronica C. Ardi, Victoria A. Johnson, Robert C. Vasko, Shelli R. McAlpine
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.
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