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Synthesis and antitumor activity of emodin quaternary ammonium salt derivatives.

Abstract：

:A series of new emodin derivatives modified at the C-3 and the C-6 positions were synthesized, and evaluated for their anticancer activities in vitro and in vivo. Among them, Compounds 5g and 5h had more significant antiproliferative ability against HepG2, BGC-823, AGS cancer cell lines and low cytotoxicity to HELF normal cell line, respectively. Compounds 5g and 5h induced AGS cell cycle arrest at G0/G1 phase and induce apoptosis via activation of caspase-3 and caspase-9 enzyme. In vivo studies using H22 xenografts in Kunming mice were conducted with 5g and 5h. The results revealed that the medium dosage group (10 mg/kg) of 5g and the high dosage group (25 mg/kg) of 5h showed significant antitumor activity compared to the control group.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Shao J,Zhang F,Bai Z,Wang C,Yuan Y,Wang W

doi

10.1016/j.ejmech.2012.07.047

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

308-19

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00473-4

journal_volume

56

pub_type

杂志文章

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