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Design, Synthesis, and Bioactivity Investigation of Tetrandrine Derivatives as Potential Anti-cancer Agents

Abstract

• Twenty four 14-sulfonamide-tetrandrine derivatives as potentially anti-cancer agents were designed and synthesized. The synthetic derivatives were investigated for their anti-cancer activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, all the compounds were determined for their IC50 values (50% inhibitory concentrations). These derivatives exhibited potent, but distinct inhibitory effects on the above mentioned cell lines. Among them, compound 23 which was modified by 2-naphthalenesulfonyl group at the 14-amino position, showed impressive inhibition on all the five cancer cell lines, especially on 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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Publication details

The article was received on 05 Mar 2018, accepted on 24 Apr 2018 and first published on 04 May 2018


Article type: Research Article
DOI: 10.1039/C8MD00125A
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Design, Synthesis, and Bioactivity Investigation of Tetrandrine Derivatives as Potential Anti-cancer Agents

    J. song, J. lan, C. chen, S. hu, J. Song, W. Liu, X. zeng, H. lou, Y. Ben-David and W. Pan, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00125A

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