نتایج جستجو برای: benzenesulfonamides

تعداد نتایج: 93  

Journal: :Chemical communications 2011
Anna Di Fiore Alfonso Maresca Vincenzo Alterio Claudiu T Supuran Giuseppina De Simone

N-substituted benzenesulfonamides, incorporating the N-amino-, N-hydroxy- and N-methoxy-moieties at the sulfonamide zinc binding group, have been investigated as CAIs by means of inhibition and structural studies, unraveling interesting aspects related to their inhibition mechanism.

2012
Kamil Brożewicz Jarosław Sławiński

ABSTRACT Two series of novel 4-chloro-2-(benzylthio)-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides and their N-aroyl derivatives have been synthesized and evaluated for in vitro anticancer activity against the full NCI-60 cell line panel. Most of the compounds exhibited antiproliferative activity. Among them a compound bearing an N-(thien-2-ylcarbonyl) moiety showed broad-spectrum activity with 5...

Journal: :iranian journal of pharmaceutical research 0
nouraddin hosseinzadeh department of medicinal chemistry, faculty of pharmacy and pharmaceutical sciences research center, tehran university of medical sciences, tehran14176, iran. soodeh seraj islamic azad university, shahre rey branch. mohamad ebrahim bakhshi-dezffoli department of medicinal chemistry, faculty of pharmacy and pharmaceutical sciences research center, tehran university of medical sciences, tehran14176, iran. mohammad hasani school of chemistry, college of science, university of tehran, tehran iran. mehdi khoshneviszadeh department of medicinal chemistry, faculty of pharmacy and pharmaceutical sciences research center, tehran university of medical sciences, tehran14176, iran. saeed fallah-bonekohal department of toxicology and pharmacology, faculty of pharmacy and laboratory of toxicology, pharmaceutical sciences research centre, tehran university of medical sciences, tehran 14155-6451, iran.

the complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. these drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems...

Journal: :Journal of medicinal chemistry 1989
M C Menziani P G De Benedetti F Gago W G Richards

Molecular mechanics methods have been applied to study the interaction between a series of 20 deprotonated benzenesulfonamides and the enzyme carbonic anhydrase. The different contributions to the binding energy have been evaluated and correlated with experimental inhibition data and molecular orbital indices of the sulfonamides in their bound conformation. The results suggest that the discrimi...

2014
Mostafa M. Ghorab Marwa G. El-Gazzar Mansour S. Alsaid

A series of 4-(substituted)-N-(guanidinyl)benzenesulfonamides bearing biologically active pyrazole, pyrimidine and pyridine moieties were prepared and evaluated for their anticancer activity against human tumor breast cell line (MCF7). These sulfonamides showed promising activity with IC50 values ranging from 49.5 to 70.2 μM. The structure-activity relationship of the synthesized compounds was ...

Journal: :Cancer cell 2016
Michaël Cerezo Abdelali Lehraiki Antoine Millet Florian Rouaud Magali Plaisant Emilie Jaune Thomas Botton Cyril Ronco Patricia Abbe Hella Amdouni Thierry Passeron Veronique Hofman Baharia Mograbi Anne-Sophie Dabert-Gay Delphine Debayle Damien Alcor Nabil Rabhi Jean-Sébastien Annicotte Laurent Héliot Mariano Gonzalez-Pisfil Caroline Robert Solange Moréra Armelle Vigouroux Philippe Gual Maruf M U Ali Corine Bertolotto Paul Hofman Robert Ballotti Rachid Benhida Stéphane Rocchi

We have discovered and developed a series of molecules (thiazole benzenesulfonamides). HA15, the lead compound of this series, displayed anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. Our molecule displayed activity against other liquid and solid tumors. HA15 also exhibited strong efficacy in x...

2010
Juan Sánchez-Cortés Katinka Bähr Milan Mrksich

This paper describes a molecular strategy to restore adhesion of cells to surfaces that otherwise do not present ligands that can mediate adhesion. The approach is based on a carbonic anhydrase fusion protein that binds benzenesulfonamides and that also includes the RGD peptide motif that can bind to cell-surface integrin adhesion receptors. In this way, the fusion protein can bind to a monolay...

2011
Sutanun Doungsoongnuen Apilak Worachartcheewan Ratchanok Pingaew Thummaruk Suksrichavalit Supaluk Prachayasittikul Somsak Ruchirawat Virapong Prachayasittikul

In the previous studies, the cytotoxicities of anthranilate sulfonamides were investigated. Herein, the bioactivities of 4-substituted (X = NO2, OCH3, CH3, Cl) benzenesulfonamides of anthranilic acid (5-8) are reported. The results revealed that all sulfonamides selectively exerted antifungal activity (25-50 % inhibition) against C. albicans at 4 μg/mL. Furthermore, compounds 6 and 8 show antio...

Journal: :Analytical chemistry 1994
F A Gomez L Z Avila Y H Chu G M Whitesides

This paper describes the estimation of binding constants (Kb) between carbonic anhydrase B (CAB, EC 4.2.1.1, from bovine erythrocytes) and charged benzenesulfonamides by affinity capillary electrophoresis (ACE) under conditions in which the migration time is affected by changes in electroosmotic flow and by nonspecific interactions accompanying changes in the concentration of ligand. Comparison...

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