A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation

CT Supuran - Bioorganic & Medicinal Chemistry Letters, 2023 - Elsevier
Advances in the carbonic anhydrase (CA, EC 4.2. 1.1) research over the last three decades
are presented, with an emphasis on the deciphering of the activation mechanism, the …

[HTML][HTML] 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 …

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 …

Design, synthesis, and biological activity of novel dithiocarbamate‐methylsulfonyl hybrids as carbonic anhydrase inhibitors

D Osmaniye, C Türkeş, Y Demir, Y Özkay… - Archiv der …, 2022 - Wiley Online Library
Carbonic anhydrase (CA) enzymes are involved in many physiological events. These
enzymes, which contain Zn2+ in their structure, can be easily inhibited by dithiocarbamate …

Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets

G Satija, B Sharma, A Madan, A Iqubal… - Journal of …, 2022 - Wiley Online Library
Benzimidazole, the benzo derivative of imidazole, is a class of bicyclic aromatic organic
compound consisting of six‐membered benzene ring fused to five‐membered imidazole at 4 …

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 …

1, 5-diaryl-1, 2, 4-triazole ureas as new SLC-0111 analogues endowed with dual carbonic anhydrase and VEGFR-2 inhibitory activities

AE Elsawi, MM Elbadawi, A Nocentini… - Journal of Medicinal …, 2023 - ACS Publications
Presently, dual targeting by a single small molecule stands out as an effective cancer-
fighting weapon. Carbonic anhydrase (CA) and vascular-endothelial growth factor (VEGF) …

Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII

T Al-Warhi, MM Elbadawi, A Bonardi… - Journal of Enzyme …, 2022 - Taylor & Francis
In this work, different series of benzothiazole-based sulphonamides 8a-c, 10, 12, 16a-b and
carboxylic acids 14a-c were developed as novel SLC-0111 analogues with the goal of …

Development of isatin-thiazolo [3, 2-a] benzimidazole hybrids as novel CDK2 inhibitors with potent in vitro apoptotic anti-proliferative activity: Synthesis, biological and …

WM Eldehna, MA El Hassab, MF Abo-Ashour… - Bioorganic …, 2021 - Elsevier
In the current medical era, human health is experiencing numerous challenges, particularly
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …

Discovery of novel pyridazine-tethered sulfonamides as carbonic anhydrase II inhibitors for the management of glaucoma

HO Tawfik, MM Saleh, A Ammara… - Journal of Medicinal …, 2024 - ACS Publications
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …