新型2,6-二取代嘌呤衍生物的合成及其抗肿瘤活性

以2,6-二氯嘌呤为原料，对其2-位和6-位进行结构修饰，合成了8个新型2,6-二胺嘌呤类衍生物(3a~3h),其结构经¹H NMR, IR和MS（ESI）表征。采用MTT法研究了3a~3h对人胃癌SGC-7901细胞的体外抗肿瘤活性。结果表明: 3a, 3b, 3c, 3g具有良好的抗肿瘤活性，其中3c（IC₅₀ 65.01 μmol·L^-1）对人胃癌细胞SGC-7901的抑制作用最强。

Synthesis and Antitumor Activities of Novel 2,6-Disubstituted Purine Derivatives

Eight novel 2,6-diamine purine derivatives were synthesized by structure-modification on 2-and 6-position of 2,6-dichloropurine.The structures were characterized by 1H NMR, IR and MS(ESI).The in vitro anti-tumor activities of 3a～3h against human gastric carcinoma cell line SGC-7901 were investigated by MTT method. The results demonstrated that 3a, 3b, 3c, 3g showed good activity and 3c exhibited best antitumor activity with IC50 of 65.01 μmol·L-1.