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

doi:10.3390/molecules200712029

Paper

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

Published Jul 1, 2015 · Krzysztof Szafrański, J. Sławiński

Molecules

14

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0

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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-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.

Study Snapshot

Novel 4-substituted pyridine-3-sulfonamides show potential anticancer activity, with the most prominent compound showing good activity and selectivity towards leukemia, colon cancer, and melanoma subpanels.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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

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