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Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.

Abstract：

:Histone deacetylases (HDACs) are zinc-dependent or NAD(+) dependent enzymes and play a critical role in the process of tumor development. Herein a series of indoline-2,3-dione derivatives have been designed and synthesized as potential HDACs inhibitors. The preliminary biological evaluation showed that most compounds synthesized have exhibited moderate Hela cell nuclear extract inhibitory activities, among which compound 25a (IC50=10.13 nM) has shown the best efficacy. The anti-proliferative activities of some of these compounds were also discussed.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Jin K,Li S,Li X,Zhang J,Xu W,Li X

doi

10.1016/j.bmc.2015.05.048

subject

Has Abstract

pub_date

2015-08-01 00:00:00

pages

4728-4736

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00470-8

journal_volume

23

pub_type

杂志文章

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