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Issue 7, 2018
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Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents

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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.

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

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Supplementary files

Article information


Submitted
05 Mar 2018
Accepted
24 Apr 2018
First published
04 May 2018

Med. Chem. Commun., 2018,9, 1131-1141
Article type
Research Article

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, 9, 1131
DOI: 10.1039/C8MD00125A

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