S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors.
Antigens, Neoplasm
/ metabolism
Carbonic Anhydrase IX
/ antagonists & inhibitors
Carbonic Anhydrase Inhibitors
/ chemical synthesis
Carbonic Anhydrases
/ metabolism
Dose-Response Relationship, Drug
Humans
Isoenzymes
/ antagonists & inhibitors
Molecular Docking Simulation
Molecular Structure
Quinazolinones
/ chemistry
Structure-Activity Relationship
Sulfonamides
/ chemistry
Metalloenzyme
molecular docking study
quinazolinone incorporating ethylsulfonamide
selectivity CA inhibitors
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2020
Dec 2020
Historique:
entrez:
20
3
2020
pubmed:
20
3
2020
medline:
28
10
2020
Statut:
ppublish
Résumé
We evaluated the hCA (CA, EC 4.2.1.1) inhibitory activity of novel 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides (compounds
Identifiants
pubmed: 32189526
doi: 10.1080/14756366.2020.1742117
pmc: PMC7144323
doi:
Substances chimiques
Antigens, Neoplasm
0
Carbonic Anhydrase Inhibitors
0
Isoenzymes
0
Quinazolinones
0
Sulfonamides
0
CA9 protein, human
EC 4.2.1.1
Carbonic Anhydrase IX
EC 4.2.1.1
Carbonic Anhydrases
EC 4.2.1.1
carbonic anhydrase XII
EC 4.2.1.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
733-743Références
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