Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine derivatives

被引：6

作者：

Guo DeXiang ^{[1
]}

Liu YaJing ^{[1
]}

Li Ting ^{[1
]}

Wang Nan ^{[1
]}

Zhai Xin ^{[1
]}

Hu Chun ^{[1
]}

Gong Ping ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab New Drugs Design & Discovery Liaoning Pro, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China

来源：

SCIENCE CHINA-CHEMISTRY | 2012年 / 55卷 / 03期

基金：

中国国家自然科学基金;

关键词：

heterocycle; synthesis; 4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine derivatives; antitumor activity;

D O I：

10.1007/s11426-011-4477-6

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new series of 4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine derivatives have been designed and synthesized. The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-(benzo[d][1,3]dioxol-5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine (CH05) (IC50 = 0.44 mu M, 3.07 mu M) was 2.0 and 8.4 times more active than gefitinib (IC50 = 0.89 mu M, 16.81 mu M) against A549 and H460 cell lines, respectively.

引用

页码：347 / 351

页数：5

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