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为了寻找具有更好抗肿瘤活性的化合物,设计合成了一系列噁唑并[5,4-d]嘧啶类衍生物。以盐酸乙脒为起始原料,合成了13个化合物8a~8m;目标化合物结构经IR、~1H NMR、EI-MS和元素分析确证;采用MTT法先后对目标化合物进行了人脐静脉内皮细胞(HUVEC)的抗肿瘤血管生成抑制活性测试和3株肿瘤细胞(A549、HepG2、U251)的体外抗肿瘤活性测试;结果表明,化合物8c、8d、8g、8i和8l对HUVEC和3株不同肿瘤细胞表现出明显的增殖抑制活性;化合物8l对A549、HepG2和U251的抑制活性略优于阳性对照药舒尼替尼,值得进一步研究。
In order to find compounds with better anti-tumor activity, a series of oxazolo [5,4-d] pyrimidine derivatives were designed and synthesized. Thirteen compounds, 8a ~ 8m, were synthesized starting from acetamidine hydrochloride. The structures of the target compounds were confirmed by IR, ~ 1H NMR, EI-MS and elemental analysis. The target compounds were treated with MTT method for human umbilical vein endothelial cells (HUVEC) and 3 tumor cells (A549, HepG2, U251) in vitro. The results showed that compounds 8c, 8d, 8g, 8i and 8l were effective against HUVEC and 3 different tumors The results showed that the inhibitory activity of compound 8 on A549, HepG2 and U251 was slightly better than that of sunitinib, which is worthy of further study.