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

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

  • Bioorg Med Chem. 2015 Aug 1;23(15):4728-4736. doi: 10.1016/j.bmc.2015.05.048.
Kang Jin 1,  Shanshan Li 1,  Xiaoguang Li 1,  Jian Zhang 1,  Wenfang Xu 2,  Xuechen Li 3
Affiliations

Affiliations

  • 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.
PMID: 26100440 DOI: 10.1016/j.bmc.2015.05.048
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.

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