4-取代-7-氯喹啉衍生物的合成及抗肿瘤活性的初步评价

Synthesis of 4-substituted-7-chloroquinoline derivatives and preliminary evaluation of their antitumor activity

目的：设计合成一系列4-取代-7-氯喹啉衍生物并测定其抗肿瘤活性。方法：4，7-二氯喹啉通过烃化反应及缩合反应得到目标化合物，并采用MTT法，评价了其对4种体外培养肿瘤细胞的生长抑制作用。结果：大多数化合物具有一定的抑制肿瘤细胞增殖的活性，其中化合物3，5和10a抑制人非小细胞肺癌A549，NCI-H446，Hela细胞生长的作用强于阳性对照，化合物5和10a对于人非小细胞肺癌A549的抑制活性是阳性对照药的4～5倍，明显优于阳性对照。结论：本文合成的该系列部分化合物具有较好的抗肿瘤活性，是潜在的抗肿瘤候选药物。

Objective： To design and synthesize a series of 4-substituted-7-chloroquinoline derivatives, and to assay their antitumor activity. Methods： The compounds were synthesized through alkylation and condensation reaction using 4,7-dichloro-quinoline, and the antitumor activities were assayed by MTT. Results： Most synthe- sized compounds had the property of antiproliferation on tumor cell lines in vitro. It was obvious that the compounds of 3,5 and 10a had stronger effect on the growth of A549, NCI-H446 and Hela cancer cells than the positive con- trol group does, and compounds 5 and 10a also showed 4 - 5 times more inhibition effect on the A549 cells than the positive control group in terms of antitumor activity. Conclusion： The series of synthesized compounds exhibit ex- cellent antitumor activities and deserve consideration for potential candidate of antitumor drugs