To investigate the cytotoxic effect and its mechanism of the micromolecule compound on the leukemia cells.The cytotoxic effects of 28 Nilotinib derivatives on K562, KA, KG, HA and 32D cell lines were detected by MTT assays, and the compound Nilo 22 was screen out. Cell apoptosis and cell cycle on leukemia cells were detected by flow cytometry. The effect of compound screened out on leukemogenesis potential of MLL-AF9 leukemia mice GFPNilo 22 serves as the most outstanding candidate out of 28 Nilotinib derivatives, which impairs leukemia cell lines, but spares normal hematopoietic cell line. Comparing with Nilotinib, Nilo 22 could induce the apoptosis of GFPNilo 22 shows a significant cytotoxic effect on mice and human leukemia cells, especially for drug resistance cells. Nilo 22 is a promising anti-leukemia agent to solve the common clinical problems of drug resistance and relapse of leukemia.探究新型端粒酶抑制剂Nilo 22对白血病细胞的杀伤作用与机制.探讨一系列人工合成的小分子化合物对白血病细胞的杀伤作用及其作用机制.采用MTT法检测28个小分子化合物对K562、KA、KG、HA及32D细胞系的杀伤作用，筛选出安全有效的化合物Nilo 22。采用流式细胞术检测该化合物对MLL-AF9小鼠白血病细胞（GFP筛选到能有效杀伤白血病细胞系且对32D细胞系相对安全的小分子化合物Nilo 22；相对于尼洛替尼，Nilo 22诱导小鼠白血病细胞凋亡的作用更加显著，轻微地阻滞细胞周期于GNilo 22对白血病细胞有显著的杀伤作用，尤其对耐药细胞有很好的杀伤效果，有望成为治疗白血病的先导化合物以解决目前临床常见的白血病耐药和复发问题.
