Synthesis and Carbonic Anhydrase I, II, IX, and XII Inhibition Studies with a Series of Cyclic Sulfonyl Guanidines.
ChemMedChem
; : e202400197, 2024 Jun 26.
Article
em En
| MEDLINE
| ID: mdl-38923747
ABSTRACT
A series of thirteen cyclic sulfonyl guanidines were prepared and evaluated against tumor-associated human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA IX and hCA XII, as well as against off-target cytosolic isoforms hCA I and hCA II. The compounds reported here were generally inactive against both off-target isoforms (KI>100â
µM), while all of them moderately inhibited both target isoforms hCA IX and XII in the submicromolar to micromolar ranges in which KI values spanned from 0.57 to 8.4â
µM against hCA IX and from 0.34 to 9.7 against hCA XII. Due to the notable selectivity of the title compounds toward isoforms hCA IX and XII, they can be considered as useful scaffolds for further chemical optimization to develop new highly selective antitumor agents.
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Idioma:
En
Revista:
ChemMedChem
Assunto da revista:
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Letônia