Organic Letters · 2005 · 36 citations · 7 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyCombinatorial ChemistryDrug DiscoveryCombinatorial SynthesisNatural Product DerivatizationNatural Product Drug DiscoveryNatural Product-based Drug DesignAmino Acid SubstitutionAnticancer ActivityAnticancer Natural ProductsChemical Synthesis Of AnaloguesMedicinal Chemistry ApplicationsSynthetic Analogues
Described are the syntheses of 14 derivatives of the natural product Sansalvamide A, where two are more active against HCT 116 colon cancer cell lines than the natural product. These derivatives were synthesized using a combinatorial-type strategy that permits elucidation of the amino acid role in the cytotoxicity, and they lay the groundwork for development of new anticancer agents. [structure: see text]
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