Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: Where are we today?

CB Mishra, M Tiwari, CT Supuran - Medicinal Research …, 2020 - Wiley Online Library
Abstract Carbonic anhydrases (CAs, EC 4.2. 1.1) are widely distributed metalloenzymes in
both prokaryotes and eukaryotes. They efficiently catalyze the reversible hydration of carbon …

Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008–2018)

A Nocentini, CT Supuran - Expert Opinion on Therapeutic Patents, 2018 - Taylor & Francis
Introduction: Human carbonic anhydrases (CA, EC 4.2. 1.1) IX and XII are tumor-associated
proteins, being part of the molecular machinery that tumor cells build as adaptive responses …

A general linear free energy relationship for predicting partition coefficients of neutral organic compounds

D Chen, Q Wang, Y Li, Y Li, H Zhou, Y Fan - Chemosphere, 2020 - Elsevier
Predicting the effects of organic compounds on environments and biological systems is an
important objective for environmental chemistry and human health. The logarithm (to base …

Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery

A Nocentini, CT Supuran - Expert Opinion on Drug Discovery, 2019 - Taylor & Francis
Introduction: Of the 15 human carbonic anhydrase (CA, EC 4.2. 1.1) isoforms known to date,
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …

A decade of tail-approach based design of selective as well as potent tumor associated carbonic anhydrase inhibitors

A Kumar, K Siwach, CT Supuran, PK Sharma - Bioorganic Chemistry, 2022 - Elsevier
Human carbonic anhydrase (hCA) isoforms hCA IX and hCA XII are well established
anticancer drug targets and their selective inhibition is highly desired for the proper …

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 …

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 …

Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail …

HO Tawfik, A Petreni, CT Supuran… - European journal of …, 2022 - Elsevier
The hydrophobic and the hydrophilic rims in the active site of human carbonic anhydrase IX
(hCA IX) which as well contains a zinc ion as part of the catalytic core, were simultaneously …

From antibacterial to antitumour agents: a brief review on the chemical and medicinal aspects of sulfonamides

H Azevedo-Barbosa, DF Dias, LL Franco… - Mini Reviews in …, 2020 - ingentaconnect.com
Sulfonamides have been in clinical use for many years, and the development of bioactive
substances containing the sulfonamide subunit has grown steadily in view of their important …

3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and …

MF Abo-Ashour, WM Eldehna, A Nocentini… - European Journal of …, 2019 - Elsevier
Herein we describe the design and synthesis of two series of sulfonamides featuring N-
unsubstituted (4a-c) or N-substituted (7a-o) isatin moieties (as tails) connected to …