title: Medicinal chemistry of Hsp90 inhibitors.
abstract: Heat shock protein (Hsp90) inhibitors are an increasingly interesting and important class of compounds where the first in class, natural product derived inhibitors such as 17-allylaminogeldanamycin (17-AAG), are entering late stage clinical development. Recently the emergence of synthetic, small molecule inhibitors has been described and both NVP-AUY922 and BIIB021 have entered clinical development. The medicinal chemistry of these and other published small molecule Hsp90 inhibitors is described in this review.
authors.affiliation: Vernalis R&D Ltd., Granta Park, Great Abington, Cambridge CB21 6GB, UK. m.drysdale@vernalis.com
authors.forename: Martin J
authors.initials: MJ
authors.lastname: Drysdale
authors.forename: Paul A
authors.initials: PA
authors.lastname: Brough
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D018841:HSP90 Heat-Shock Proteins / Q000037:antagonists & inhibitors*; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D018841:HSP90 Heat-Shock Proteins