title: 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.
authors.affiliation: Department of Chemistry and Biochemistry, San Diego State University, San Diego, CA 92182-1030, USA.
authors.forename: Leslie D
authors.initials: LD
authors.lastname: Alexander
authors.forename: Robert P
authors.initials: RP
authors.lastname: Sellers
authors.forename: Melinda R
authors.initials: MR
authors.lastname: Davis
authors.forename: Veronica C
authors.initials: VC
authors.lastname: Ardi
authors.forename: Victoria A
authors.initials: VA
authors.lastname: Johnson
authors.forename: Robert C
authors.initials: RC
authors.lastname: Vasko
authors.forename: Shelli R
authors.initials: SR
authors.lastname: McAlpine
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047630:Depsipeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016503:Drug Delivery Systems; D018841:HSP90 Heat-Shock Proteins / Q000037:antagonists & inhibitors; D006367:HeLa Cells; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D018841:HSP90 Heat-Shock Proteins; C119376:sansalvamide A