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Vorinostat-like molecules as structural, stereochemical, and pharmacological tools

Hanessian, Stephen and Auzzas, Luciana and Larsson, Andreas and Zhang, Jianbin and Giannini, Giuseppe and Gallo, Grazia and Ciacci, Andrea and Cabri, Walter (2010) Vorinostat-like molecules as structural, stereochemical, and pharmacological tools. ACS Medicinal Chemistry Letters, Vol. 1 (2), p. 70-74. ISSN 1948-5875. Article.

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DOI: 10.1021/ml100028g


The inhibitory activity of an ω-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.

Item Type:Article
ID Code:5796
Uncontrolled Keywords:HDAC promiscuous inhibitors, SAHA analogues, HDAC1−11 profile, class IIa-specific profile, absorption and metabolism
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Divisions:002 Altri enti e centri di ricerca del Nord Sardegna > CNR-Consiglio Nazionale delle Ricerche > Istituto di chimica biomolecolare, Sassari
Publisher:American Chemical Society
Deposited On:11 May 2011 09:39

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