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合成、表征、新型含喹啉尾巴吡唑啉衍生物的抗阿米巴活性和细胞毒性。

Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail.

机构信息

Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.

出版信息

Eur J Med Chem. 2010 Oct;45(10):4669-75. doi: 10.1016/j.ejmech.2010.07.028. Epub 2010 Jul 23.

Abstract

The cyclization of chalcones (1a-1j) with 2-(quinolin-8-yloxy) acetohydrazide (2) under basic condition led to the formation of new compounds, pyrazoline derivatives (3a-3j). In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that the compounds 3d, 3g, 3h, and 3j exhibited promising antiamoebic activity (IC(50) = 0.05 microM, 0.31 microM, 0.06 microM, 0.29 microM) respectively than the standard drug metronidazole (IC(50) = 1.84 microM). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds 3d, 3g, 3h, 3j and metronidazole were nontoxic at the concentration range of 1.56-50 microM.

摘要

查耳酮(1a-1j)与 2-(8-喹啉氧基)乙酰胺肼(2)在碱性条件下环化,生成新的化合物,吡唑啉衍生物(3a-3j)。对希氏内阿米巴 HM1:IMSS 株进行了体外抗阿米巴活性测试。结果表明,化合物 3d、3g、3h 和 3j 表现出有希望的抗阿米巴活性(IC50 = 0.05μM、0.31μM、0.06μM、0.29μM),分别优于标准药物甲硝唑(IC50 = 1.84μM)。这些化合物对人乳腺癌 MCF-7 细胞系的毒理学研究表明,化合物 3d、3g、3h、3j 和甲硝唑在 1.56-50μM 的浓度范围内均无毒性。

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