新型三环肟醚衍生物的合成及其抗肿瘤活性  

Synthesis and antitumor activities of novel tricyclic oximino derivatives

作　　者：郭淑春[1] 陈阳[1] 张珂良 王伟[1] 李伟[1] 宫平[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]辽宁省食品药品监督管理局技术审评中心,辽宁沈阳110003

出　　处：《中国药物化学杂志》2007年第5期274-278,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成8H-噻吩并[2,3-b]吡咯里嗪-8-肟醚类化合物,并对其体外抗肿瘤活性进行初步评价。方法以芳基乙腈为原料,经多步反应合成目标化合物;采用MTT法,以顺铂为阳性对照药,以Bel-7402和HT-1080为测试细胞株对目标化合物的抗肿瘤活性进行了评价。结果与结论合成了12个新化合物,经1H-NMR、MS和IR确认其结构。体外活性实验表明:化合物7d显示出较好的抗肿瘤活性。Aim To design and synthesize a series of novel thieno [ 2, 3-b] pyrrolizine derivatives, and to evaluate their antitumor activities. Methods Twelve target compounds were synthesized in several steps with the starting material arylacetonitrile and their antitumor activities were examined against Bel-7402 and HT1080 cell lines in vitro with cisplatin as positive control. Results and conclusion The structures of twelve new compounds were confirmed by 1H-NMR, IR, and MS. The pharmacological tests showed that compound 7d showed promising antitumor activity.

关 键 词：8H-噻吩并[2 3-b]吡咯里嗪类化合物 抗肿瘤活性 微管蛋白抑制剂 

分 类 号：R914[医药卫生—药物化学]