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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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.
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