2. Academic Validation
  3. Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents

Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents

  • Medchemcomm. 2018 May 4;9(7):1131-1141. doi: 10.1039/c8md00125a.
Junrong Song 1 2,  Junjie Lan 2 3,  Chao Chen 2 3,  Shengcao Hu 3 4,  Jialei Song 2 3,  Wulin Liu 2 3,  Xueyi Zeng 2 3,  Huayong Lou 2 3,  Yaacov Ben-David 2 3,  Weidong Pan 1 2 3
Affiliations

Affiliations

  • 1 Guizhou University , Huaxi Avenue South , Guiyang 550025 , PR China . Email: wdpan@163.com.
  • 2 State Key Laboratory of Functions and Applications of Medicinal Plants , Guizhou Medical University , 3491 Baijin Road , Guiyang 550014 , PR China . Email: yaacovbendavid@hotmail.com.
  • 3 The Key Laboratory of Chemistry for Natural Products of Guizhou Province and , Chinese Academy of Sciences , 3491 Baijin Road , Guiyang 550014 , PR China.
  • 4 Zunyi Medical University , 6 West Road , Zunyi 563000 , PR China.
PMID: 30109000 DOI: 10.1039/c8md00125a
Abstract

Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic derivatives were investigated for their cytotoxic activity against human Cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all of the compounds were determined. These derivatives exhibited potent, but distinct, inhibitory effects on the above-mentioned cell lines. Among them, compound 23, which was modified with a 2-naphthalenesulfonyl group at the 14-amino position, showed impressive inhibition of all five Cancer cell lines, and especially of MDA-MB-231 cells with an IC50 value of 1.18 ± 0.14 μM. Further mechanism exploration showed that 23 induced potent apoptotic cell death on MDA-MB-231 Cancer cells in a concentration-dependent manner. The results revealed that 23 might be a potential anti-cancer drug candidate.

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