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.
Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools / Hanessian S; Auzzas L; Larsson A; Zhang JB; Giannini G; Gallo G; Ciacci A; Cabri W. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - ELETTRONICO. - 1:2(2010), pp. 70-74. [10.1021/ml100028g]
Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools
Cabri W
2010
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.