title: Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.
abstract: Heat shock protein 90 is emerging as an important target in cancer chemotherapy. In a program directed toward identifying novel chemical probes for Hsp90, we found N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)benzene sulfonamide as an Hsp90 inhibitor with very weak activity. In this report, we present a new and general method for the synthesis of a variety of analogs around this scaffold, and discuss their structure-activity relationships.
authors.affiliation: Chemical Biology Discovery Center, Emory University, 1510 Clifton Road, Atlanta, GA 30322, USA. tganesh@emory.edu
authors.forename: Thota
authors.initials: T
authors.lastname: Ganesh
authors.forename: Pahk
authors.initials: P
authors.lastname: Thepchatri
authors.forename: Lian
authors.initials: L
authors.lastname: Li
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Du
authors.forename: Haian
authors.initials: H
authors.lastname: Fu
authors.forename: James P
authors.initials: JP
authors.lastname: Snyder
authors.forename: Aiming
authors.initials: A
authors.lastname: Sun