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

查看全文 作　　者：GUO [1]DeXiang;LIU [1]YaJing;LI [1]Ting;WANG [1]Nan;ZHAI [1]Xin;HU [1]Chun;GONG [1]Ping

机构地区：[1]Key Laboratory of New Drugs Design and Discovery of Liaoning Province,School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China

出　　处：《Science China Chemistry》索引2012年第55卷第3期,共5页

基　　金：supported by the National Natural Science Foundation of China (20474053) 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]dioxol5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine (CH05) (IC50=0.44 M,3.07 M) was 2.0 and 8.4 times more active than gefitinib (IC50=0.89 M,16.81 M) against A549 and H460 cell lines,respectively. 关键词：抗肿瘤活性嘧啶衍生物二氢合成肿瘤细胞株 A549细胞 IC50 化合物

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

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