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

Molecules

Krzysztof Szafrański¹  Jarosᐪw Sᐪwiński¹ 

关键词: sulfonamides;    pyridine-3-sulfonamides;    sulfonylureas;    diarylsulfonylureas;    anticancer;    antitumor activity;   

DOI  :  10.3390/molecules200712029

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.