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新型二取代蒽作为一种抗结肠癌的有效药物。

Novel disubstituted chrysene as a potent agent against colon cancer.

作者信息

Banik Bimal K, Basu Manas K, Becker Fredrick F

机构信息

Department of Chemistry, The University of Texas-Pan American, 1201 West University Drive, Edinburg, TX 78539.

出版信息

Oncol Lett. 2010 Nov;1(6):1033-1035. doi: 10.3892/ol.2010.167. Epub 2010 Sep 8.

Abstract

Research on polycyclic aromatic hydrocarbons and their derivatives has received significant attention from the scientific community. The present study involved the synthesis of several novel 6,12-disubstituted chrysene derivatives. Nitration of chrysene with nitric acid produced 6,12-dinitrochrysene which when reduced yielded 6,12-diaminochrysene. A coupling reaction of 6,12-diaminochrysene with an acid in the presence of isobutylchloroformate produced amide. The reduction of amide produced an amine. The amino was converted to a hydrochloride salt. The new compounds were characterized through different types of analytical data. One of these compounds demonstrated marked activity in vivo against a colon cancer cell line. Inhibition of the growth of this tumor was best noted at day 20 when each treatment regimen inhibited the average tumor volume by 50%. In a number of in vivo tests in various regimens, the hydrochloride salt demonstrated consistent inhibition of the growth of the cancer HT-29 cell line. Despite the research progress in polycyclic aromatic compounds, the use of these types of molecules as anticancer agents has not been reported systematically.

摘要

多环芳烃及其衍生物的研究已受到科学界的高度关注。本研究涉及几种新型6,12 - 二取代屈衍生物的合成。用硝酸对屈进行硝化反应生成6,12 - 二硝基屈,将其还原后得到6,12 - 二氨基屈。在异丁基氯甲酸酯存在下,6,12 - 二氨基屈与一种酸发生偶联反应生成酰胺。酰胺还原生成胺。氨基被转化为盐酸盐。通过不同类型的分析数据对新化合物进行了表征。其中一种化合物在体内对结肠癌细胞系表现出显著活性。在第20天时,每种治疗方案对肿瘤平均体积的抑制率达50%,此时对该肿瘤生长的抑制最为明显。在多种方案的一系列体内试验中,盐酸盐对癌症HT - 29细胞系的生长表现出持续的抑制作用。尽管多环芳烃化合物的研究取得了进展,但尚未有系统报道将这类分子用作抗癌剂的情况。

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引用本文的文献

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