1.
Curr Top Med Chem
; 21(31): 2767-2770, 2021.
Artigo
em Inglês
| MEDLINE
| ID: mdl-34607543
2.
J Enzyme Inhib Med Chem
; 36(1): 1874-1883, 2021 Dec.
Artigo
em Inglês
| MEDLINE
| ID: mdl-34340614
RESUMO
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.