2. Academic Validation
  3. Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors

Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors

  • Bioorg Med Chem. 2016 Sep 15;24(18):4120-4128. doi: 10.1016/j.bmc.2016.06.054.
Liping Wang 1,  Rong Wu 1,  Wenwei Fu 1,  Yuanzhi Lao 1,  Changwu Zheng 1,  Hongsheng Tan 2,  Hongxi Xu 3
Affiliations

Affiliations

  • 1 School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Cai Lun Lu 1200, Shanghai 201203, People's Republic of China; Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, People's Republic of China.
  • 2 School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Cai Lun Lu 1200, Shanghai 201203, People's Republic of China; Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, People's Republic of China. Electronic address: ths97029@163.com.
  • 3 School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Cai Lun Lu 1200, Shanghai 201203, People's Republic of China; Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, People's Republic of China. Electronic address: xuhongxi88@gmail.com.
PMID: 27396929 DOI: 10.1016/j.bmc.2016.06.054
Abstract

Oblongifolin C, one of the polyprenylated benzoylphloroglucinol Natural Products (PPAPs) isolated from the fruits of Garcinia yunnanensis Hu, was recently discovered to be a potent anti-tumor agent. A collection of 12 derivatives with modifications on the benzophenone moieties were synthesized and tested for c-Met kinase inhibition and cytotoxicity against the HepG2, Miapaca-2, HCC827, Hela, A549, AGS, and HT-29 cell lines in vitro. An oxidized derivative, 10, was found to possess strong inhibition and anti-migration properties in the HCC827 cell line and serves as a potential lead compound for the development of new Anticancer drugs. In addition, structure-activity relationships (SAR) were also evaluated to provide key information for future Anticancer drug development.

Keywords

Cytotoxicity; Derivatives; HCC827 cell line; Modification; Oblongifolin C; Structure–activity relationships; c-Met kinase inhibitor.

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