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Molecules 2015, 20(7), 12029-12044; doi:10.3390/molecules200712029

Synthesis of Novel 1-(4-Substituted pyridine-3-sulfonyl)-3-phenylureas with Potential Anticancer Activity

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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Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 2 April 2015 / Revised: 16 June 2015 / Accepted: 24 June 2015 / Published: 1 July 2015
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Abstract

A series of novel 4-substituted-N-(phenylcarbamoyl)-3-pyridinesulfonamides 1127 have been synthesized by the reaction of 4-substituted pyridine-3-sulfonamides 210 with the appropriate aryl isocyanates in presence of potassium carbonate. The in vitro anticancer activity of compounds 11, 12, 1421 and 2426 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-chlorophenyl)carbamoyl]-4-[4-(3,4-dichlorophenyl)piperazin-1-yl]pyridine-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
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Szafrański, K.; Sławiński, J. Synthesis of Novel 1-(4-Substituted pyridine-3-sulfonyl)-3-phenylureas with Potential Anticancer Activity. Molecules 2015, 20, 12029-12044.

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