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新型含生物活性磺酰胺基的喹啉和嘧啶并[4,5-b]喹啉类抗肿瘤药物。

Novel quinolines and pyrimido[4,5-b]quinolines bearing biologically active sulfonamide moiety as a new class of antitumor agents.

机构信息

Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.

出版信息

Eur J Med Chem. 2010 Feb;45(2):738-44. doi: 10.1016/j.ejmech.2009.11.021. Epub 2009 Nov 18.

DOI:10.1016/j.ejmech.2009.11.021
PMID:19944497
Abstract

Some novel quinolines and pyrimido[4,5-b]quinolines have been synthesized. The structures of which were confirmed by elemental analyses and spectral data. All the target compounds were subjected to in-vitro antitumor activity against Ehrlich Ascites Carcinoma (EAC) cells. Compounds 24, 19 and 12 showed higher activity with IC(50) values (5.5, 6.9, 7 microg/ml) when compared with Doxorubicin as a reference drug (IC(50) value 38 microg/ml).

摘要

一些新型喹啉和嘧啶并[4,5-b]喹啉已经被合成。其结构通过元素分析和光谱数据得到确认。所有的目标化合物都进行了体外抗肿瘤活性测试,针对的是艾氏腹水癌细胞(EAC)。与阿霉素(IC50 值为 38μg/ml)作为参比药物相比,化合物 24、19 和 12 的活性更高,IC50 值分别为 5.5、6.9 和 7μg/ml。

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