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新型细胞毒剂2-氨基-4-(硝基烷基)-4H-色烯-3-腈类化合物

2-Amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles as New Cytotoxic Agents.

作者信息

Zonouzi Afsaneh, Mirzazadeh Roghieh, Safavi Maliheh, Kabudanian Ardestani Sussan, Emami Saeed, Foroumadi Alireza

机构信息

School of Chemistry, University College of Science, University of Tehran, P.O. Box 14155- 6455, Tehran, Iran.

Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2013 Fall;12(4):679-85.

Abstract

A series of 2-amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles were synthesized by an efficient multicomponent reaction in aqueous media using DBU as a catalyst at room temperature. Mild condition, environment friendly procedure and excellent yields are the main advantages of this procedure. The cytotoxic activity of target compounds were evaluated against three cancer cell lines MDA-MB-231, MCF-7 and T47D in comparison with etoposide as reference drug. Generally, all compounds showed good cell growth inhibitory activity with IC(50) values less than 30 μg/mL. Their activities were comparable or more potent than standard drug etoposide. The 6-bromo- derivatives 7e and 7f showed promising cytotoxic activity with IC50 values in the range of 3.46-18.76 μg/mL, being more potent than etoposide against all tested cell lines.

摘要

在室温下,以DBU为催化剂,通过在水介质中进行高效多组分反应,合成了一系列2-氨基-4-(硝基烷基)-4H-色烯-3-腈。温和的条件、环境友好的方法和优异的产率是该方法的主要优点。与作为参考药物的依托泊苷相比,评估了目标化合物对三种癌细胞系MDA-MB-231、MCF-7和T47D的细胞毒性活性。一般来说,所有化合物都表现出良好的细胞生长抑制活性,IC(50)值小于30μg/mL。它们的活性与标准药物依托泊苷相当或更强。6-溴衍生物7e和7f表现出有前景的细胞毒性活性,IC50值在3.46-18.76μg/mL范围内,对所有测试细胞系的活性均比依托泊苷更强。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/29cf/3920703/35d30af336fb/ijpr-12-679-g001.jpg

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