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新型达沙替尼衍生物的设计、合成及体外抗增殖活性。

Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives.

机构信息

School of Chemistry and Chemical Engineering, Institute of Pharmaceutical Engineering, Southeast University, 87 Dingjiaqiao, Nanjing, Jiangsu 210096, PR China.

出版信息

Bioorg Med Chem Lett. 2012 Jan 15;22(2):806-10. doi: 10.1016/j.bmcl.2011.12.070. Epub 2011 Dec 20.

Abstract

Two series of novel Dasatinib derivatives have been designed and synthesized, with their in vitro cytostatic effect screened on human chronic myeloid leukemia cell line K562 and human myeloid leukemia cell line U937. Some target compounds demonstrated significant inhibitory activities against both cell lines. Compared to the contrast drug Dasatinib, 1b, 1c, 1d, 1e and 1f were found to demonstrate more potent antitumor activities. The structures of all the newly synthesized compounds were determined by (1)H NMR and (13)C NMR.

摘要

已经设计和合成了两系列新型达沙替尼衍生物,并在体外对人慢性髓系白血病细胞系 K562 和人髓样白血病细胞系 U937 进行了细胞抑制作用的筛选。一些目标化合物对这两种细胞系均显示出显著的抑制活性。与对照药物达沙替尼相比,发现 1b、1c、1d、1e 和 1f 具有更强的抗肿瘤活性。所有新合成化合物的结构均通过 1H NMR 和 13C NMR 确定。

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