Search results for "Drug Design"

showing 2 items of 232 documents

Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of t…

2009

The biological importance of microtubules in mitosis and cell division makes them an interesting target for the development of anticancer agents. Small molecules such as benzo[b]furans are attractive as inhibitors of tubulin polymerization. Thus, a new class of inhibitors of tubulin polymerization based on the 2-(3′,4′,5′-trimethoxybenzoyl)-benzo[b]furan molecular skeleton, with electron-donating (Me, OMe or OH) or electron-withdrawing (F, Cl and Br) substituents on the benzene ring, was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization and cell cycle effects. Adding a methyl group at the C-3 position resulted in increased activity. The most prom…

structure-activityStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic Agentsmacromolecular substancesBiochemistryChemical synthesisArticleStructure-Activity Relationshipchemistry.chemical_compoundbenzo[b]furansMicrotubuleCell Line TumorFuranDrug DiscoveryHumansStructure–activity relationshipMolecular BiologyBenzofuransCell ProliferationBinding SitesDose-Response Relationship DrugbiologyChemistryTubulin ModulatorsCell growthCell CycleOrganic ChemistrySmall moleculeTubulin Modulatorstubulin polymerizationTubulinDrug Designbiology.proteinMolecular MedicineProtein MultimerizationColchicine
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Sulfonamide moiety as "molecular chimera" in the design of new drugs.

2021

Background: The -SO2NH- group is of great significance in modern pharmaceutical use since, in sulfa-drugs, it is possible to introduce easily chemical modifications, and even small changes may lead to an improved version of an already existing drug. Objective: This paper aims to describe updated information in the sulfonamide field with a particular focus on new mechanisms of action, especially if discovered by employing computational approaches. Methods: Research articles that focused on the use of the sulfonamide moiety for the design, synthesis, and in vitro/in vivo tests of various diseases were collected from various search engines like PubMed, Science Direct, Google Scholar, and Scop…

sulfonamide moietyPharmacologyOrganic Chemistrymolecular chimeraSettore CHIM/08 - Chimica FarmaceuticaBiochemistrymolecular dynamicsin silico drug designdockingDrug Discoverypharmacophore modelingMolecular Medicinealkylsulfonamidesaryl/heteroarylsulfonamidesCurrent medicinal chemistry
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