2. Academic Validation
  3. Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance

Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance

  • Eur J Med Chem. 2018 May 25:152:516-526. doi: 10.1016/j.ejmech.2018.05.003.
Yong Li 1,  Wei Yan 1,  Jianhong Yang 1,  Zhuang Yang 1,  Mengshi Hu 1,  Peng Bai 1,  Minghai Tang 1,  Lijuan Chen 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, Sichuan, 610041, China.
  • 2 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, Sichuan, 610041, China. Electronic address: chenlijuan125@163.com.
PMID: 29754076 DOI: 10.1016/j.ejmech.2018.05.003
Abstract

Twenty-four novel β-carboline/acylhydrazone hybrids were synthesized and evaluated for their in vitro antiproliferative activity. Among them, 12r exhibited the most potent activity, with IC50 values of 1-2 μM against panel of Cancer cell lines and retained significant activity in multidrug resistant Cancer cells. Treated cells were not arrested in any phase of cell cycle but resulted in late cellular Apoptosis on both MCF-7 and MCF-7/ADR Cancer cells. Importantly, 12r showed certain antitumor effect on inhibiting the tumor growth with low toxic and side effects and without significant body weight loss.

Keywords

Antitumor activity; Cellular apoptosis; H460 xenograft model; Multidrug resistance; β-Carboline.

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