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Novel disubstituted chrysene as a potent agent against colon cancer.
Oncology Letters ( IF 2.5 ) Pub Date : 2010-09-08 , DOI: 10.3892/ol.2010.167 Bimal K Banik 1 , Manas K Basu , Fredrick F Becker
Oncology Letters ( IF 2.5 ) Pub Date : 2010-09-08 , DOI: 10.3892/ol.2010.167 Bimal K Banik 1 , Manas K Basu , Fredrick F Becker
Affiliation
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.
中文翻译:
新型二取代 chrysene 作为抗结肠癌的有效药物。
多环芳烃及其衍生物的研究受到科学界的极大关注。本研究涉及几种新型 6,12-二取代 chrysene 衍生物的合成。用硝酸硝化屈产生 6,12-二硝基屈,当还原生成 6,12-二氨基屈时。在氯甲酸异丁酯存在下,6,12-二氨基屈与酸的偶联反应产生酰胺。酰胺的还原产生胺。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显示出显着的活性。在第 20 天,当每种治疗方案将平均肿瘤体积抑制了 50% 时,这种肿瘤生长的抑制作用最为明显。在不同方案的许多体内试验中,盐酸盐显示出对癌症 HT-29 细胞系生长的一致抑制。尽管多环芳族化合物的研究取得了进展,但尚未系统地报道将这些类型的分子用作抗癌剂。
更新日期:2019-11-01
中文翻译:
新型二取代 chrysene 作为抗结肠癌的有效药物。
多环芳烃及其衍生物的研究受到科学界的极大关注。本研究涉及几种新型 6,12-二取代 chrysene 衍生物的合成。用硝酸硝化屈产生 6,12-二硝基屈,当还原生成 6,12-二氨基屈时。在氯甲酸异丁酯存在下,6,12-二氨基屈与酸的偶联反应产生酰胺。酰胺的还原产生胺。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显示出显着的活性。在第 20 天,当每种治疗方案将平均肿瘤体积抑制了 50% 时,这种肿瘤生长的抑制作用最为明显。在不同方案的许多体内试验中,盐酸盐显示出对癌症 HT-29 细胞系生长的一致抑制。尽管多环芳族化合物的研究取得了进展,但尚未系统地报道将这些类型的分子用作抗癌剂。