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N-双(三氟甲基)烷基-N'-噻唑基和 N-双(三氟甲基)烷基-N'-苯并噻唑基脲的合成及抗癌活性。

Synthesis and anticancer activity of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and N-bis(trifluoromethyl)alkyl-N'-benzothiazolyl ureas.

机构信息

Institute of Physiologically Active Compounds, Severnyi pr. 1, Chernogolovka, Moscow region 142432, Russia.

出版信息

Eur J Med Chem. 2009 Dec;44(12):4944-53. doi: 10.1016/j.ejmech.2009.08.007. Epub 2009 Aug 28.

Abstract

A number of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and -benzothiazolyl ureas have been synthesized and evaluated for their in vitro antiproliferative activities against the human cancer cell lines at the National Cancer Institute (NCI, USA). The activity was shown for compounds 8a,c and 9a-c. The most sensitive cell lines relative to the tested compounds are: 8c PC-3 (prostate cancer, logGI(50) -7.10), 9c SNB-75 (CNS cancer, logGI(50) -5.84), 9b UO-31 (renal cancer, logGI(50) -5.66), and SR (leukemia, logGI(50) -5.44) human cancer cells.

摘要

已经合成了一系列 N-双(三氟甲基)烷基-N'-噻唑基和 -苯并噻唑基脲,并在美国国立癌症研究所(NCI)评估了它们对人类癌细胞系的体外抗增殖活性。显示出化合物 8a、c 和 9a-c 的活性。相对于测试化合物最敏感的细胞系是:8c PC-3(前列腺癌,logGI(50)-7.10)、9c SNB-75(中枢神经系统癌症,logGI(50)-5.84)、9b UO-31(肾癌,logGI(50)-5.66)和 SR(白血病,logGI(50)-5.44)人类癌细胞。

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