Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies.
J Enzyme Inhib Med Chem
; 36(1): 1874-1883, 2021 Dec.
Article
en En
| MEDLINE
| ID: mdl-34340614
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.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Quinazolinas
/
Sulfonamidas
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Inhibidores de Anhidrasa Carbónica
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Biología Computacional
/
Isoenzimas
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2021
Tipo del documento:
Article
País de afiliación:
Italia