新型2-(4-喹啉/喹唑啉)硫代苯并噻唑类化合物的合成与抗肿瘤活性的评价
Synthesis and preliminary evaluation of novel 2-(quinolin-4-ylthio) benzothiazole derivatives as potential anticancer agents
作者：李潇;赵立峰;刘志昊;余洛汀;
Author：
收稿日期： 年卷（期）页码：2013,28(06):-560-562
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：2-巯基苯并噻唑;喹啉;结构拼合;抗肿瘤活性;黑色素瘤
Key words：
基金项目：
中文摘要
目的设计并制备了11个新型2-(4-喹啉/喹唑)啉硫代-6-氨基苯并噻唑类化合物,并探讨其抗肿瘤活性。方法依据拼合原理,将2-巯基-6-氨基苯并噻唑和4-氯-6,7-二甲氧基喹唑啉(或喹啉)两个片段结合,形成关键结构并据此合成系列衍生物,用MTT法进行体外抗肿瘤活性评价和构效关系研究。结果与结论合成的11个新化合物Ia~Ik未见文献报道;其中化合物Ic对黑色素瘤细胞株A2058的IC50为21.2μmol·L-1(Sorafenib 23.5μmol·L-1);化合物Ib、Ic对黑色素瘤细胞株A875的IC50分别为25.4、27.0μmol·L-1(Sorafenib 28.5μmol·L-1),显示的活性均优于阳性对照药物,但对测试的其他肿瘤细胞株均未显示活性。
参考文献
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