埃罗替尼衍生物的合成及抗肿瘤活性

目的:设计和合成出新的喹唑啉类化合物并研究其抗肿瘤活性.方法:3,4一二甲氧基苯甲酸乙酯经过醚化,再依次经过硝化、还原、环舍得到4一氯.6,7-二(2.甲氧基乙氧基)]-3H-喹唑啉-4-酮,最后氯代、与间氨基苯乙炔缩合、水解制得抗肿瘤药埃罗替尼,或者与氨基衍生物炔缩合、水解生成目标化合物.按MTY方法测定了目标化合物抗肿瘤活性.结果和结论:合成了8个埃罗替尼衍生物(8a-8h),其结构经核磁、质谱和红外光谱等数据确证.初步的抗肿瘤活性研究表明:在对人肺癌细胞A549的体外生长抑制作用上,所合成化合物对人肺癌细胞A549均具有一定程度的抑制作用,其中,化合物8a、8c和8h活性与吉非替尼和埃罗替尼相当.

Synthesis and antitumor activities of erlotinib derivatives

Aim:To study the synthesis and antitumor activities of erlotinib derivatives.Methods:Erlotinib derivatives were synthesized from ethyl 3,4-dimethoxybenzoate via etherification,nitrification,reduction,and then cyclization to afford 4-chloro-6,7-di(2-methoxyethoxy)quinazolin-4-one,which was finally subjected to chlorination and condensation with 3-aminophenylacetylene or other aminoderivatives.Percentage of inhibition on the antitumor growth was measured using MTT method.Results and Conclusion:Eight compound...