3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity

被引：0
|
作者：
Khaled A. M. Abouzid
Nadia A. Khalil
Eman M. Ahmed
Khaled Omar Mohamed
机构：
[1] Faculty of Pharmacy,Pharmaceutical Chemistry Department
[2] Ain Shams University,Pharmaceutical Organic Chemistry Department
[3] Faculty of Pharmacy,undefined
[4] Cairo University,undefined
来源：
Archives of Pharmacal Research | 2013年 / 36卷
关键词：
Pyridazine; Colon cancer; Vatalanib; Cytotoxic;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC50 values equal to 15.3 and 3.9 μM respectively. The most promising compound, 2b, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.
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页码：41 / 50
页数：9
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