Title of article :
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
Author/Authors :
Thota Ganesh، نويسنده , , Pahk Thepchatri، نويسنده , , Lian Li، نويسنده , , Yuhong Du، نويسنده , , Haian Fu، نويسنده , , James P. Snyder، نويسنده , , Aiming Sun، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
6
From page :
4982
To page :
4987
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.
Keywords :
structure-based design , FP assay , antiproliferative activity , Suzuki-coupling , Heat shock protein 90 , sulfonamides
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2008
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
799931
Link To Document :
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