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Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors.

ABSTRACT: Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

SUBMITTER: Zhang JH

PROVIDER: S-EPMC7607388 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors.

Zhang Jie-Huan JH Mottamal Madhusoodanan M Jin Hai-Shan HS Guo Shanchun S Gu Yan Y Wang Guangdi G Zhao Li-Ming LM

Future medicinal chemistry 20191108 21

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative ...[more]

PMID: 31702394

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