Synthesis of flavonoids nitrogen mustard derivatives and study on their antitumor activity in vitro.

Xi Yan, Jinglei Song, Meixuan Yu, Hao-Ling Sun, Haijun Hao

Bioorganic chemistry 2020 Mar

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Several novel flavonoids nitrogen mustard derivatives were synthesized and evaluated for antiproliferative activity against seven human cancer cell lines (HeLa, A549, HepG2, MCF7, SH-SY5Y, PC-3, DU145) by the MTT assay in vitro. The resulting IC50 showed that most compounds exhibited better inhibitory activity against seven cell lines. IC50 values of some compounds were lower than well-known melphalan. In particular, compound 8b was the most promising compound which inhibited HeLa cells with IC50 value of 1.43 μM. It showed excellent antitumor activity against these seven cell lines. Besides, it could arrest cell cycle of HeLa in G2/M phase and induce cell apoptosis. The loss of mitochondrial membrane potential may be an apoptotic mediating factor. Copyright © 2020 Elsevier Inc. All rights reserved.

Citation

Xi Yan, Jinglei Song, Meixuan Yu, Hao-Ling Sun, Haijun Hao. Synthesis of flavonoids nitrogen mustard derivatives and study on their antitumor activity in vitro. Bioorganic chemistry. 2020 Mar;96:103613