Title of article
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors
Author/Authors
David M. Andrews، نويسنده , , Elaine S.E. Stokes، نويسنده , , Greg R. Carr، نويسنده , , Zbigniew S. Matusiak، نويسنده , , Craig A. Roberts ، نويسنده , , Michael J. Waring، نويسنده , , Madeleine C. Brady، نويسنده , , Christine M. Chresta، نويسنده , , Simon J. East، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
2580
To page
2584
Abstract
A lead benzamide, 3, was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Optimization led to 16d, demonstrating an excellent balance of efficacy and non-efficacy properties, along with very desirable in vivo DMPK. The final compounds presented are >1000-fold more potent than the initial screen hit, an improvement in potency which was achieved with a concomitant significant improvement in all the main non-efficacy properties.
Keywords
Benzamide , HDAC , Histone , Deacetylase , anticancer
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799404
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