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Keywords = pyridinesulfonamide

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13 pages, 3273 KiB  
Communication
Synthesis, Crystal Structure, Absolute Configuration and Antitumor Activity of the Enantiomers of 5-Bromo-2-chloro-N-(1-phenylethyl)pyridine-3-sulfonamide
by Zhixu Zhou, Linwei Li, Ning Yan, Lei Du, Changshan Sun and Tiemin Sun
Molecules 2015, 20(11), 20926-20938; https://doi.org/10.3390/molecules201119740 - 24 Nov 2015
Cited by 5 | Viewed by 6255
Abstract
Pyridinesulfonamide is an important fragment which has a wide range of applications in novel drugs. R- and S-isomers of 5-bromo-2-chloro-N-(1-phenylethyl)pyridine-3-sulfonamide have been synthesized, and the stereostructures have been researched. Single crystals of both compounds were obtained for X-ray analysis, [...] Read more.
Pyridinesulfonamide is an important fragment which has a wide range of applications in novel drugs. R- and S-isomers of 5-bromo-2-chloro-N-(1-phenylethyl)pyridine-3-sulfonamide have been synthesized, and the stereostructures have been researched. Single crystals of both compounds were obtained for X-ray analysis, and the absolute configurations (ACs) have been further confirmed by electronic circular dichroism (ECD), optical rotation (OR) and quantum chemical calculations. The crystal structures and calculated geometries were extremely similar, which permitted a comparison of the relative reliabilities of ACs obtained by ECD analyses and theoretical simulation. In addition, the effect of stereochemistry on the PI3Kα kinase and anticancer activity were investigated. Compounds 10a and 10b inhibit the activity of PI3Kα kinase with IC50 values of 1.08 and 2.69 μM, respectively. Furthermore, molecular docking was performed to analyze the binding modes of R- and S-isomers. Full article
(This article belongs to the Section Medicinal Chemistry)
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16 pages, 779 KiB  
Article
Synthesis of Novel 1-(4-Substituted pyridine-3-sulfonyl)-3-phenylureas with Potential Anticancer Activity
by Krzysztof Szafrański and Jarosław Sławiński
Molecules 2015, 20(7), 12029-12044; https://doi.org/10.3390/molecules200712029 - 1 Jul 2015
Cited by 18 | Viewed by 7236
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, [...] Read more.
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. Full article
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