Release Time:2019-03-13  Hits:

Indexed by: Journal Article

Date of Publication: 2016-04-13

Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Included Journals: Scopus、PubMed、SCIE

Volume: 112

Page Number: 196-208

ISSN: 0223-5234

Key Words: Flavone; Phosphoramidate; HepG2; G2/M arrest; Apoptosis

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 mu mol/L, 5.5 mu mol/L and 6.6 mu mol/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. (C) 2016 Elsevier Masson SAS. All rights reserved.