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Bioorg Med Chem. 2015 Aug 1;23(15):4728-36. doi: 10.1016/j.bmc.2015.05.048. Epub 2015 Jun 3.

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

Author information

1
Department of Medicinal Chemistry, School of Pharmacy, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan, Shandong 250012, PR China.
2
Department of Medicinal Chemistry, School of Pharmacy, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan, Shandong 250012, PR China. Electronic address: wfxu@yahoo.cn.
3
Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, PR China. Electronic address: xuechenl@hku.hk.

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.

KEYWORDS:

Biological evaluation; HDAC inhibitors; Indoline-2,3-dione derivatives; QSAR; Synthesis

PMID:
26100440
DOI:
10.1016/j.bmc.2015.05.048
[Indexed for MEDLINE]

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