2. Academic Validation
  3. Design, synthesis and biological evaluation of a series of pyrano chalcone derivatives containing indole moiety as novel anti-tubulin agents

Design, synthesis and biological evaluation of a series of pyrano chalcone derivatives containing indole moiety as novel anti-tubulin agents

  • Bioorg Med Chem. 2014 Apr 1;22(7):2060-79. doi: 10.1016/j.bmc.2014.02.028.
Guangcheng Wang 1,  Chunyan Li 1,  Lin He 1,  Kai Lei 1,  Fang Wang 1,  Yuzi Pu 1,  Zhuang Yang 2,  Dong Cao 1,  Liang Ma 1,  Jinying Chen 1,  Yun Sang 2,  Xiaolin Liang 1,  Mingli Xiang 1,  Aihua Peng 1,  Yuquan Wei 1,  Lijuan Chen 3
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.
  • 2 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 610064, Sichuan, China.
  • 3 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: 24629450 DOI: 10.1016/j.bmc.2014.02.028
Abstract

A new series of pyrano chalcone derivatives containing indole moiety (3-42, 49a-49r) were synthesized and evaluated for their antiproliferative activities. Among all the compounds, compound 49b with a propionyloxy group at the 4-position of the left phenyl ring and N-methyl-5-indoly on the right ring displayed the most potent cytotoxic activity against all tested Cancer cell lines including multidrug resistant phenotype, which inhibits Cancer cell growth with IC50 values ranging from 0.22 to 1.80μM. Furthermore, 49b significantly induced cell cycle arrest in G2/M phase and inhibited the polymerization of tubulin. Molecular docking analysis demonstrated the interaction of 49b at the colchicine binding site of tubulin. In experiments in vivo, 49b exerted potent Anticancer activity in HepG2 human liver carcinoma in BALB/c nude mice. These results indicated these compounds are promising inhibitors of tubulin polymerization for the potential treatment of Cancer.

Keywords

Chalcone; Indole; Millepachine; Tubulin.

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