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

• 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.

Nyckelord

HDAC promiscuous inhibitors

SAHA analogues

HDAC1-11 profile

class IIa-specific profile

absorption and metabolism

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