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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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2805559PMC
http://dx.doi.org/10.1021/jm901566cDOI Listing

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