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KMID : 0043320130360010041
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Archives of Pharmacal Research
2013 Volume.36 No. 1 p.41 ~ p.50
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3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity
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Abouzid Khaled A. M.
Khalil Nadia A.
Ahmed Eman M.
Mohamed Khaled Omar
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Abstract
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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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KEYWORD
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Pyridazine, Colon cancer, Vatalanib, Cytotoxic
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