[HTML][HTML] An overview of coumarin as a versatile and readily accessible scaffold with broad-ranging biological activities

F Annunziata, C Pinna, S Dallavalle… - International Journal of …, 2020 - mdpi.com
Privileged structures have been widely used as an effective template for the research and
discovery of high value chemicals. Coumarin is a simple scaffold widespread in Nature and …

Emerging role of carbonic anhydrase inhibitors

CT Supuran - Clinical Science, 2021 - portlandpress.com
Inhibition of carbonic anhydrase (CA, EC 4.2. 1.1) was clinically exploited for decades, as
most modern diuretics were obtained considering as lead molecule acetazolamide, the …

Carbonic anhydrase inhibitors targeting metabolism and tumor microenvironment

A Angeli, F Carta, A Nocentini, JY Winum… - Metabolites, 2020 - mdpi.com
The tumor microenvironment is crucial for the growth of cancer cells, triggering particular
biochemical and physiological changes, which frequently influence the outcome of …

Exploring the multiple binding modes of inhibitors to carbonic anhydrases for novel drug discovery

CT Supuran - Expert opinion on drug discovery, 2020 - Taylor & Francis
Introduction The spacious active site cavity of the metalloenzyme carbonic anhydrase (CA,
EC 4.2. 1.1) shows a great versatility for a variety of binding modes for modulators of activity …

Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase

A Nocentini, A Angeli, F Carta, JY Winum… - Journal of Enzyme …, 2021 - Taylor & Francis
Inorganic anions inhibit the metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1) generally
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …

Experimental carbonic anhydrase inhibitors for the treatment of hypoxic tumors

CT Supuran - Journal of Experimental Pharmacology, 2020 - Taylor & Francis
Abstract Carbonic anhydrase (CA, EC 4.2. 1.1) isoforms IX and XII are overexpressed in
many hypoxic tumors as a consequence of the hypoxia inducible factor (HIF) activation …

Sulfonamide inhibitors of human carbonic anhydrases designed through a three-tails approach: improving ligand/isoform matching and selectivity of action

A Bonardi, A Nocentini, S Bua, J Combs… - Journal of medicinal …, 2020 - ACS Publications
The “tail approach” has become a milestone in human carbonic anhydrase inhibitor (hCAI)
design for various therapeutics, including antiglaucoma agents. Besides the classical …

Multi-and poly-pharmacology of carbonic anhydrase inhibitors

CT Supuran - Pharmacological reviews, 2024 - Elsevier
Eight genetically distinct families of the enzyme carbonic anhydrase (CA, EC 4.2. 1.1) were
described in organisms allover the phylogenetic tree. They catalyze the hydration of CO 2 to …

Carbonic anhydrase inhibition by antiviral drugs in vitro and in silico

C Türkeş - Journal of Molecular Recognition, 2023 - Wiley Online Library
Enzyme inhibition is a commonly utilized method for controlling enzymatic activity in various
physiologically relevant biological systems. Herein, the selected five active antiviral drugs …

Novel carbonic anhydrase inhibitors with dual-tail core sulfonamide show potent and lasting effects for glaucoma therapy

A Angeli, I Chelli, L Lucarini… - Journal of Medicinal …, 2024 - ACS Publications
Glaucoma, a leading cause of irreversible vision loss worldwide, is characterized by
elevated intraocular pressure (IOP), a well-established risk factor across all its forms. We …