Synthesis of Novel 1-4-Substituted pyridine-3-sulfonyl-3-phenylureas with Potential Anticancer ActivityReport as inadecuate




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Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland



These authors contributed equally to this work.





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Academic Editor: Jean Jacques Vanden Eynde

Abstract A series of novel 4-substituted-N-phenylcarbamoyl-3-pyridinesulfonamides 11–27 have been synthesized by the reaction of 4-substituted pyridine-3-sulfonamides 2–10 with the appropriate aryl isocyanates in presence of potassium carbonate. The in vitro anticancer activity of compounds 11, 12, 14–21 and 24–26 was evaluated at the U.S. National Cancer Institute and in light of the results, some structure-activity relationships were discussed. The most prominent compound, N-4-chlorophenylcarbamoyl-4-4-3,4-dichlorophenylpiperazin-1-ylpyridine-3-sulfonamide 21 has exhibited a good activity profile and selectivity toward the subpanels of leukemia, colon cancer and melanoma, with average GI50 values ranging from 13.6 to 14.9 µM. View Full-Text

Keywords: sulfonamides; pyridine-3-sulfonamides; sulfonylureas; diarylsulfonylureas; anticancer; antitumor activity sulfonamides; pyridine-3-sulfonamides; sulfonylureas; diarylsulfonylureas; anticancer; antitumor activity





Author: Krzysztof Szafrański † and Jarosław Sławiński †,*

Source: http://mdpi.com/



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