中文摘要：

本文合成了一系列新结构的2-（1-取代哌啶-4-氨基）喹唑啉衍生物，采用MTT法评价了化合物对5种肿瘤细胞系的抑制活性。研究结果表明：在哌啶环上引入小体积的疏水性烷基取代基，得到的化合物4j-41、5a、5b和5d具有较强的细胞毒活性，IC50值在微摩尔水平。在小鼠移植瘤模型实验中，化合物41表现出了较强的体内抗肿瘤活性，在200mg·kg-1的剂量下，对H22肿瘤生长抑制率为72．9％，对Lewis肺癌的抑制率达到了80％。

英文摘要：

A variety of novel 2-（1-substituted-piperidine-4-ylamino）quinazoline derivatives were prepared and their antiproliferative activities on five cancer cell lines were evaluated by MTT assay. Quinazolines 4j-41, 5a, 5b and 5d bearing a small hydrophobic alkyl group on piperidine ring exhibited potent antitumor activities with ICs0 values at micromolar level. Compound 41 displayed significant in vivo antitumor activity with 72.9% inhibition on H22 tumor growth and 80% inhibition on Lewis lung cancer growth at a dose of 200 mg kg-1.