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以邻甲基苯胺、3-乙酰基吡啶、N,N二甲基甲酰胺二甲基缩醛为起始原料,经硝化、加成、环合、还原、缩合等6步反应合成目标化合物。以伊马替尼为阳性对照药,采用台盼蓝排染法,以慢性粒细胞白血病K562细胞为测试细胞株,对目标化合物进行体外抗白血病活性评价。所合成的18个化合物结构经1HNMR和MS确证。初步药理实验结果表明,目标化合物对K562细胞有一定的抗肿瘤活性,但低于阳性对照药伊马替尼和先导化合物。酰胺键结构对保持活性有重要的影响,是药物与受体的重要结合位点。
The target compounds were synthesized by o-methylaniline, 3-acetylpyridine and N, N-dimethylformamide dimethyl acetal using nitration, addition, cyclization, reduction and condensation reactions. To Imatinib as positive control drug, using trypan blue exclusion method, with chronic myeloid leukemia K562 cells as test cell lines, the target compound for anti-leukemia activity evaluation. The structures of the 18 compounds synthesized were confirmed by 1H NMR and MS. Preliminary pharmacological experiments show that the target compound has certain anti-tumor activity on K562 cells, but lower than the positive control drug imatinib and lead compounds. The amide bond structure has an important influence on the retention activity and is an important binding site for the drug and the receptor.