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新型二芳基脲衍生物的设计、合成及体外抗肿瘤活性评价。

Design, synthesis, and in vitro antitumor evaluation of novel diaryl ureas derivatives.

机构信息

Pharmaceutical Engineering Institute, School of Chemistry & Chemical Engineering, Southeast University, Nanjing 210096, PR China.

出版信息

Eur J Med Chem. 2010 Jun;45(6):2299-306. doi: 10.1016/j.ejmech.2010.02.005. Epub 2010 Feb 6.

Abstract

Two series of novel diaryl ureas have been designed and synthesized, with their in vitro antitumor effect screened on human non-small cell lung cancer (NSCLC) cell line A549 and human breast cancer cell line MDA-MB-231. Some target compounds demonstrated significant inhibitory activities against both cell lines. Compared to contrast drug Sorafenib, 1b, 1d, 1f, 1i were found to demonstrate more potent antitumor activities. The structures of all the newly synthesized compounds were determined by 1H, 13C NMR, MS, IR and elementary analysis.

摘要

已经设计和合成了两个系列的新型二芳基脲,并在人非小细胞肺癌(NSCLC)细胞系 A549 和人乳腺癌细胞系 MDA-MB-231 上筛选了其体外抗肿瘤活性。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。与对照药物索拉非尼相比,发现 1b、1d、1f、1i 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、13C NMR、MS、IR 和元素分析确定。

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