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. 2014 Oct 30;86:639-52.
doi: 10.1016/j.ejmech.2014.09.024. Epub 2014 Sep 8.

Design, Synthesis, and Biological Evaluation of 1, 3-disubstituted-pyrazole Derivatives as New Class I and IIb Histone Deacetylase Inhibitors

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Design, Synthesis, and Biological Evaluation of 1, 3-disubstituted-pyrazole Derivatives as New Class I and IIb Histone Deacetylase Inhibitors

Yiwu Yao et al. Eur J Med Chem. .

Abstract

A novel series of HDAC inhibitors demonstrating class I and IIb subtype selectivity have been identified using a scaffold-hopping strategy. Several designed compounds showed better selectivity for class I and IIb over class IIa HDAC isoforms comparing to the FDA approved HDAC targeting drug SAHA. A representative lead compound 22 bearing a biphenyl moiety demonstrated promising class I and IIb HDAC isoforms selectivity and in vitro anticancer activities against several cancer cell lines. This work could serve as a fundamental platform for further exploration of selective HDAC inhibitors using designed molecular scaffold.

Keywords: HDAC; Isoforms selectivity; Scaffold-hopping; Structure–activity relationship.

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