Synthesis and antitumor activity of novel dithiocarbamate substituted chromones
Synthesis and antitumor activity of novel dithiocarbamate substituted chromones
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DOI：
10.1016/j.ejmech.2009.04.004
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发表时间：
2009-09-01
影响因子：
6.7
通讯作者：
Yang, Guang-Fu
中科院分区：
文献类型：
--
作者：
Huang, Wei;Ding, Yu;Yang, Guang-Fu
设计并合成了一系列带有不同二硫代氨基甲酸酯基团的色酮衍生物。采用MTT法测定其对HCCLM-7、Hela、MDA-MB-435 S、SW-480、Hep-2和MCF-7的体外抗肿瘤活性。两种化合物（3-氯-4-氧代-4H-色烯-2-基）甲基哌啶-1-硫代甲酸酯（Iq）和（6-氯-4-氧代-4H-色烯-3-基）甲基哌啶-1-硫代甲酸酯（IIu）由于其高效和广谱而被鉴定为最有希望的候选物。流式细胞仪分析表明，化合物Iq和IIu可使SW-480和MDA-MB-435细胞周期阻滞于G（2）/M期，并呈剂量依赖性，可能具有诱导肿瘤细胞凋亡的作用。(C)2009年Elsevier Masson SAS。All rights reserved.
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.