Title of article
Novel thiol-based TACE inhibitors: Rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
Author/Authors
B. Govinda Rao، نويسنده , , Upul K. Bandarage، نويسنده , , Tiansheng Wang، نويسنده , , Jon H. Come، نويسنده , , Emanuele Perola، نويسنده , , Yunyi Wei، نويسنده , , Shi-Kai Tian، نويسنده , , Jeffrey O. Saunders، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
2250
To page
2253
Abstract
A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 4b has shown excellent in vitro potency against the isolated TACE enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 4b bound to TACE was obtained.
Keywords
rheumatoid arthritis , hydroxamates , thiols , TACE inhibitors , MMP selectivity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798020
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