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Selective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 685-692. - Publication Year :
- 2021
-
Abstract
- A small library of coumarin and their psoralen analogues EMAC10157a-b-d-g and EMAC10160a-b-d-g has been designed and synthesised to investigate the effect of structural modifications on their inhibition ability and selectivity profile towards carbonic anhydrase isoforms I, II, IX, and XII. None of the new compounds exhibited activity towards hCA I and II isozymes. Conversely, both coumarin and psoralen derivatives were active against tumour associated isoforms IX and XII in the low micromolar or nanomolar range of concentration. These data further corroborate our previous findings on analogous derivatives, confirming that both coumarins and psoralens are interesting scaffolds for the design of isozyme selective hCA inhibitors.
- Subjects :
- Antigens, Neoplasm metabolism
Carbonic Anhydrase IX metabolism
Carbonic Anhydrase Inhibitors chemical synthesis
Carbonic Anhydrase Inhibitors chemistry
Coumarins chemical synthesis
Coumarins chemistry
Dose-Response Relationship, Drug
Ficusin chemical synthesis
Ficusin chemistry
Humans
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Carbonic Anhydrase IX antagonists & inhibitors
Carbonic Anhydrase Inhibitors pharmacology
Carbonic Anhydrases metabolism
Coumarins pharmacology
Ficusin pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 36
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 33602041
- Full Text :
- https://doi.org/10.1080/14756366.2021.1887171