Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools

Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools
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DOI:
10.1021/ml100028g
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发表时间:
2010-05-01
影响因子:
4.2
通讯作者:
Cabri, Walter
Cabri, Walter
中科院分区:
医学3区
文献类型:
--
作者:
Hanessian, Stephen;Auzzas, Luciana;Cabri, Walter

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The inhibitory activity of an omega-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile.