To investigate the method of synthesizing purine derivatives and their preliminary antitumor activity,purine derivatives are synthesized from 2,6-Dichloropurine through three step reactions,i.e.,substitution,bromination and condensation.The inhibitory effects of purine derivatives on the cell proliferation of human liver cancer cell HepG2 are evaluated via cell counting kit 8 (CCK8) method.The structure-activity relationships of purine derivatives are studied.Seventeen derivatives have been obtained and their chemical structures are confirmed by 1HNMR,MS and elemental analysis.The preliminary antitumor experiments indicate that the seventeen derivatives all have certain antitumor activities.Thereinto,the derivatives replaced by R-2-amino butanol at the second,3-fluorine benzyl amine at the sixth,and ethyl at the ninth position induce better antitumor effect.It is Conclused that purine derivatives possess the potent antitumor activities.%研究嘌呤衍生物的合成方法,初步探讨其体外抗肿瘤活性.以2,6-二氯嘌呤为原料,经取代、溴代、缩合,制备其衍生物；以人的肝癌细胞HepG2为模型,采用细胞计数试剂盒(CCK8)评价其抗肿瘤活性,并进行初步的构效关系研究.结果合成了17个嘌呤衍生物,结构经1H-NMR,MS和元素分析确证；初步的抗肿瘤活性实验表明所合成的化合物均有一定的抗肿瘤作用,其中2位为R-2-氨基丁醇取代、6位为3-氟苄基取代、9位为乙基取代时抗肿瘤活性较好.说明嘌呤衍生物具有潜在的抗肿瘤活性.
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