2. Academic Validation
  3. Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents

Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents

  • Bioorg Med Chem Lett. 2014 Jul 15;24(14):3158-63. doi: 10.1016/j.bmcl.2014.04.121.
Guangcheng Wang 1,  Fang Wang 2,  Dong Cao 2,  Yibin Liu 2,  Ronghong Zhang 2,  Haoyu Ye 2,  Xiuxia Li 2,  Lin He 2,  Zhuang Yang 3,  Liang Ma 2,  Aihua Peng 2,  Mingli Xiang 2,  Yuquan Wei 2,  Lijuan Chen 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China; College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China.
  • 2 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
  • 3 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China; College of Chemistry of Sichuan University, Chengdu, Sichuan 610064, China.
  • 4 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China. Electronic address: chenlijuan125@163.com.
PMID: 24863745 DOI: 10.1016/j.bmcl.2014.04.121
Abstract

A series of barbigerone analogues (7a-7w, 13a-13x) were designed, synthesized and biologically evaluated for their anti-proliferative and anti-angiogenic activities. Among these compounds, compound 13a exhibited the most potent inhibitory effect on the proliferation of HUVECs, HepG2, A375, U251, B16, and HCT116 cells (IC50=3.80, 0.28, 1.58, 3.50, 1.09 and 0.68 μM, respectively). Compound 13a inhibited the angiogenesis in zebrafish embryo assay in a concentration-dependent manner. Furthermore, 13a also effectively inhibited the migration and capillary like tube formation of human umbilical vein endothelial cell in vitro. These results support the further investigation of this class of compounds as potential anti-proliferative and anti-angiogenesis agents.

Keywords

Anti-angiogenesis; Anti-proliferative; Barbigerone; Isoflavone.

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