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

作　　者：GUO DeXiang LIU YaJing LI Ting WANG Nan ZHAI Xin HU Chun GONG 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》2012年第3期347-351,共5页中国科学（化学英文版）

基　　金：supported by the National Natural Science Foundation of China (20474053)

摘　　要：A new series of 4,5-dihydro-lH-thiochromeno[4,3-d]pyrimidine derivatives have been designed and synthesized. The anti- tumor 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-l-yl）-4,5-dihydro-1H-thiochromeno[4,3-d]pyrimidine （CH05） （IC50 = 0.44 μM, 3.07 μM） was 2.0 and 8.4 times more active than gefitinib （IC50= 0.89 μM, 16.81 μM） against A549 and H460 cell lines, respectively.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：HETEROCYCLE SYNTHESIS 4 5-dihydro-lH-thiochromeno[4 3-d]pyrimidine derivatives antitumor activity 

分 类 号：TQ463.5[化学工程—制药化工] S831.5[农业科学—畜牧学]