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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.

SUBMITTER: Alexander LD 

PROVIDER: S-EPMC2805559 | biostudies-literature | 2009 Dec

REPOSITORIES: biostudies-literature

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Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action.

Alexander Leslie D LD   Sellers Robert P RP   Davis Melinda R MR   Ardi Veronica C VC   Johnson Victoria A VA   Vasko Robert C RC   McAlpine Shelli R SR  

Journal of medicinal chemistry 20091201 24

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. ...[more]

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