Title of article
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones
Author/Authors
Upul K. Bandarage، نويسنده , , Tiansheng Wang، نويسنده , , Jon H. Come، نويسنده , , Emanuele Perola، نويسنده , , Yunyi Wei، نويسنده , , B. Govinda Rao، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
44
To page
48
Abstract
A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained.
Keywords
sulfones , TACE inhibitors , MMP selectivity , rheumatoid arthritis , hydroxamates
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798917
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