Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines

European Journal of Medicinal Chemistry
Yue-Qing LiWei-Jie Zhao

Abstract

A series of flavone-7-phosphoramidate derivatives were synthesized and tested for their antiproliferative activity in vitro against human hepatoma cell line HepG2 and human normal hepatic cell line L-O2. Compound 8d, 16d and 17d, incorporating the amino acid alanine, exhibited high inhibitory activity on HepG2 cell line with IC50 values of 9.0 μmol/L, 5.5 μmol/L and 6.6 μmol/L. The introduction of acyl groups played a pivotal role in the selective inhibition toward human hepatoma HepG2 cells, except for compound 8a, 9a and 16b. Compound 8d, 16d and 17d could significantly induce G2/M arrest in HepG2 cells. Specially, Compound 16d could lead early apoptosis in HepG2 cells.

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Citations

May 6, 2019·Cancers·Samantha Kah Ling OngAnupam Bishayee
Jul 25, 2021·International Journal of Molecular Sciences·Robert ReibergerAleš Machara

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