Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents. Issue 7 (14th June 2018)

• Record Type: Journal Article
• Authors: Song, Junrong; Lan, Junjie; Chen, Chao; Hu, Shengcao; Song, Jialei; Liu, Wulin; Zeng, Xueyi; Lou, Huayong; Ben-David, Yaacov; Pan, Weidong
• Is Part Of: MedChemComm. Volume 9:Issue 7(2018)
• Page Start: 1131
• Page End: 1141
• Publication Date: 2018-06-14
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c8md00125a
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : Twenty-four 14-sulfonamide–tetrandrine derivatives were synthesized. Compound23 exhibited growth inhibition of MDA-MB-231 cells with an IC50 value of 1.18 ± 0.14 μM. 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, compound23, 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 that23 induced potent apoptotic cell death on MDA-MB-231 cancer cells in a concentration-dependent manner. The results revealed that23 might be a potential anti-cancer drug candidate.