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Your search keyword '"Viviano, Monica"' showing total 4 results
Start Over Author "Viviano, Monica" Topic sulfonamides
4 results on '"Viviano, Monica"'

1. Discovery of Benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain.

Author

Cipriano A, Milite C, Feoli A, Viviano M, Pepe G, Campiglia P, Sarno G, Picaud S, Imaide S, Makukhin N, Filippakopoulos P, Ciulli A, Castellano S, and Sbardella G

Subjects
Male, Humans, Benzo(a)pyrene, Transcription Factors metabolism, Imidazoles pharmacology, Benzimidazoles pharmacology, Cell Cycle Proteins metabolism, Sulfonamides pharmacology, Nuclear Proteins
Abstract

The bromodomain and extra-terminal (BET) family of proteins includes BRD2, BRD3, BRD4, and the testis-specific protein, BRDT, each containing two N-terminal tandem bromodomain (BRD) modules. Potent and selective inhibitors targeting the two bromodomains are required to elucidate their biological role(s), with potential clinical applications. In this study, we designed and synthesized a series of benzimidazole-6-sulfonamides starting from the azobenzene compounds MS436 (7 a) and MS611 (7 b) that exhibited preference for the first (BD1) over the second (BD2) BRD of BET family members. The most-promising compound (9 a) showed good binding potency and improved metabolic stability and selectivity towards BD1 with respect to the parent compounds., (© 2022 The Authors. ChemMedChem published by Wiley-VCH GmbH.)

Published
2022
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2. Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies.

Author

Baglini E, Ravichandran R, Berrino E, Salerno S, Barresi E, Marini AM, Viviano M, Castellano S, Da Settimo F, Supuran CT, Cosconati S, and Taliani S

Subjects
Carbon-13 Magnetic Resonance Spectroscopy, Carbonic Anhydrase Inhibitors chemical synthesis, Carbonic Anhydrase Inhibitors chemistry, Drug Evaluation, Preclinical, Molecular Docking Simulation, Proton Magnetic Resonance Spectroscopy, Structure-Activity Relationship, Sulfonamides chemistry, Carbonic Anhydrase Inhibitors pharmacology, Computational Biology methods, Isoenzymes antagonists & inhibitors, Quinazolines chemistry, Sulfonamides pharmacology
Abstract

A library of variously decorated N -phenyl secondary sulphonamides featuring the bicyclic tetrahydroquinazole scaffold was synthesised and biologically evaluated for their inhibitory activity against human carbonic anhydrase (hCA) I, II, IV, and IX. Of note, several compounds were identified showing submicromolar potency and excellent selectivity for the tumour-related hCA IX isoform. Structure-activity relationship data attained for various substitutions were rationalised by molecular modelling studies in terms of both inhibitory activity and selectivity.

Published
2021
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3. Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold.

Author

Salerno S, Amendola G, Angeli A, Baglini E, Barresi E, Marini AM, Ravichandran R, Viviano M, Castellano S, Novellino E, Da Settimo F, Supuran CT, Cosconati S, and Taliani S

Subjects
Bridged Bicyclo Compounds, Heterocyclic chemistry, Carbonic Anhydrase Inhibitors chemical synthesis, Carbonic Anhydrase Inhibitors chemistry, Dose-Response Relationship, Drug, Humans, Indazoles chemistry, Isoenzymes antagonists & inhibitors, Isoenzymes metabolism, Models, Molecular, Molecular Structure, Structure-Activity Relationship, Sulfonamides chemical synthesis, Sulfonamides chemistry, Bridged Bicyclo Compounds, Heterocyclic pharmacology, Carbonic Anhydrase Inhibitors pharmacology, Carbonic Anhydrases metabolism, Indazoles pharmacology, Sulfonamides pharmacology
Abstract

Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the discovery of potential drugs devoid of off-target side effects. As a consequence, substantial efforts are still needed to allow for the full realization of the pharmacological potential of CA modulators. In this contribution, starting from our previous studies, we describe the synthesis of a set of new bicyclic tetrahydroindazoles featuring a secondary sulfonamide. Biological evaluation of the inhibitory activity against the hCA I, II, IV, and IX isoforms allowed drawing a structure-activity relationship profile that was rationalized through theoretical studies. This allowed dissecting the new molecules into the single portions influencing the zinc chelation properties and the selectivity profile thereby offering a new platform for the discovery of new isotype selective CA inhibitors., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2021 Elsevier Masson SAS. All rights reserved.)

Published
2021
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4. Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold

Author

Federico Da Settimo, Claudiu T. Supuran, Ettore Novellino, Sabrina Castellano, Emma Baglini, Andrea Angeli, Silvia Salerno, Rahul Ravichandran, Monica Viviano, Elisabetta Barresi, Anna Maria Marini, Giorgio Amendola, Sabrina Taliani, Sandro Cosconati, Salerno, Silvia, Amendola, Giorgio, Angeli, Andrea, Baglini, Emma, Barresi, Elisabetta, Marini, Anna Maria, Ravichandran, Rahul, Viviano, Monica, Castellano, Sabrina, Novellino, Ettore, Da Settimo, Federico, Supuran, Claudiu T, Cosconati, Sandro, and Taliani, Sabrina

Subjects
Models, Molecular, Gene isoform, Scaffold, Indazoles, Stereochemistry, Structure-activity relationships, 01 natural sciences, Structure-Activity Relationship, Secondary sulfonamides, 03 medical and health sciences, Secondary sulfonamides Carbonic anhydrase inhibitors Structure-activity relationships, Carbonic anhydrase, Carbonic anhydrase inhibitors, Drug Discovery, Humans, Chelation, Secondary sulfonamide, Carbonic anhydrase inhibitor, Carbonic Anhydrases, 030304 developmental biology, Pharmacology, chemistry.chemical_classification, Sulfonamides, 0303 health sciences, Dose-Response Relationship, Drug, Molecular Structure, biology, Bicyclic molecule, 010405 organic chemistry, Organic Chemistry, General Medicine, Bridged Bicyclo Compounds, Heterocyclic, 0104 chemical sciences, Sulfonamide, Isoenzymes, Enzyme, chemistry, biology.protein, High homology
Abstract

Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the discovery of potential drugs devoid of off-target side effects. As a consequence, substantial efforts are still needed to allow for the full realization of the pharmacological potential of CA modulators. In this contribution, starting from our previous studies, we describe the synthesis of a set of new bicyclic tetrahydroindazoles featuring a secondary sulfonamide. Biological evaluation of the inhibitory activity against the hCA I, II, IV, and IX isoforms allowed drawing a structure-activity relationship profile that was rationalized through theoretical studies. This allowed dissecting the new molecules into the single portions influencing the zinc chelation properties and the selectivity profile thereby offering a new platform for the discovery of new isotype selective CA inhibitors. Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the discovery of potential drugs devoid of off-target side effects. As a consequence, substantial efforts are still needed to allow for the full realization of the pharmacological potential of CA modulators. In this contribution, starting from our previous studies, we describe the synthesis of a set of new bicyclic tetrahydroindazoles featuring a secondary sulfonamide. Biological evaluation of the inhibitory activity against the hCA I, II, IV, and IX isoforms allowed drawing a structure-activity relationship profile that was rationalized through theoretical studies. This allowed dissecting the new molecules into the single portions influencing the zinc chelation properties and the selectivity profile thereby offering a new platform for the discovery of new isotype selective CA inhibitors.

Published
2021

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