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以2,4-二氯-5-硝基嘧啶为起始原料,通过多步反应制备了一系列新型嘌呤-8-酮衍生物,并经~1HNMR、~(13)CNMR和HRMS结构确认.采用四甲基偶氮唑盐(MTT)法测定了目标化合物的体外抗肿瘤细胞增殖活性,结果表明:部分目标化合物具有较好的抗肿瘤细胞增殖活性,其中四个化合物抑制人子宫颈癌细胞(Hela)、人急性淋巴母细胞白血病细胞(MOLT-4)和白血病细胞(K562)的活性相当或优于阳性对照药R-Roscovitine.
A series of novel purin-8-one derivatives were prepared by multistage reaction using 2,4-dichloro-5-nitropyrimidine as starting material and confirmed by ~ 1H NMR, ~ (13) CNMR and HRMS structures. The anti-tumor cell proliferation activity of the target compounds was determined by MTT assay. The results showed that some of the target compounds had good anti-tumor cell proliferation activity, of which four compounds inhibited human cervical cancer cells Hela, human acute lymphoblastic leukemia cells (MOLT-4) and leukemia cells (K562) were comparable or superior to the positive control R-Roscovitine.