Synthesis and antitumor activity of novel dithiocarbamate substituted chromones

被引：191

作者：

Huang, Wei ^{[2
]}

Ding, Yu ^{[2
]}

Miao, Yan ^{[2
]}

Liu, Ming-Zhen ^{[2
]}

Li, Yan ^{[1
]}

Yang, Guang-Fu ^{[2
]}

机构：

[1] Wuhan Univ, Zhongnan Hosp, Ctr Canc, Wuhan 430072, Peoples R China

[2] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 09期

关键词：

Flavonoids; Chromone; Dithiocarbamate; Antitumor activity; 2-METHYLCHROMONES; FLAVONOIDS;

D O I：

10.1016/j.ejmech.2009.04.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of chromone derivatives bearing diverse dithiocarbamate moieties were designed and synthesized via a three-component reaction protocol. Their in vitro antitumor activities were evaluated by MTT method against HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2 and MCF-7. Two compounds (3-chloro-4-oxo-4H-chromen-2-yl)methyl piperidine-1-carbodithioate (Iq) and (6-chloro-4-oxo-4H-chromen-3yl)methyl piperidine-1-carbodithioate (IIu), were identified as the most promising candidate due to their high potency and broad-spectrum. Further flow-activated cell sorting analysis revealed that compounds Iq and IIu arrest the cell cycle of SW-480 and MDA-MB-435s both in G(2)/M phase with dose-dependent effect and might display apoptosis-inducing effect on these tumor cell lines. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：3687 / 3696

页数：10

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