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 …

Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities

CT Supuran - Journal of Enzyme Inhibition and Medicinal …, 2022 - Taylor & Francis
The mitochondrial isoforms VA/VB of metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1)
are involved in metabolic processes, such as de novo lipogenesis and fatty acid …

Novel beta-lactam substituted benzenesulfonamides: in vitro enzyme inhibition, cytotoxic activity and in silico interactions

Ö Güleç, C Türkeş, M Arslan, Y Demir… - Journal of …, 2023 - Taylor & Francis
In this study, a library of twelve beta-lactam-substituted benzenesulfonamides (5a–l) was
synthesized using the tail-approach method. The compounds were characterized using IR …

Targeting carbonic anhydrases for the management of hypoxic metastatic tumors

CT Supuran - Expert Opinion on Therapeutic Patents, 2023 - Taylor & Francis
Introduction Several isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1)
are connected with tumorigenesis. Hypoxic tumors overexpress CA IX and XII as a …

Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications

A Angeli, CT Supuran - Journal of Enzyme Inhibition and Medicinal …, 2023 - Taylor & Francis
Click chemistry reactions constitute an important and relatively new approach in the
medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms …

Design and synthesis of 6-arylpyridine-tethered sulfonamides as novel selective inhibitors of carbonic anhydrase IX with promising antitumor features toward the …

WM Eldehna, EE Mohammed, GH Al-Ansary… - European Journal of …, 2023 - Elsevier
Hypoxia, a characteristic feature of solid tumors, develops as a result of excessive cell
proliferation and rapid tumor growth exceeding the oxygen supply, and can result in …

Development of benzene and benzothiazole-sulfonamide analogues as selective inhibitors of the tumor-associated carbonic anhydrase IX

S Manzoor, A Angeli, S Zara, S Carradori… - European Journal of …, 2022 - Elsevier
With an aim to develop novel potential antitumor agents, two series of benzene-and
benzothiazole-sulfonamide derivatives, acting as effective human carbonic anhydrase (hCA …

PET radiotracers and fluorescent probes for imaging human carbonic anhydrase IX and XII in hypoxic tumors

SG Nerella, P Singh, PS Thacker, M Arifuddin… - Bioorganic …, 2023 - Elsevier
Positron emission tomography (PET) and fluorescent imaging play a pivotal role in medical
diagnosis, biomedical oncologic research, and drug development process, which include …

Small structural differences govern the carbonic anhydrase II inhibition activity of cytotoxic triterpene acetazolamide conjugates

TC Denner, N Heise, J Zacharias, O Kraft, S Hoenke… - Molecules, 2023 - mdpi.com
Acetylated triterpenoids betulin, oleanolic acid, ursolic acid, and glycyrrhetinic acid were
converted into their succinyl-spacered acetazolamide conjugates. These conjugates were …

[HTML][HTML] Tumor associated carbonic anhydrase inhibitors: rational approaches, design strategies, structure activity relationship and mechanistic insights

SG Nerella, PS Thacker, M Arifuddin… - European Journal of …, 2024 - Elsevier
The emergence of tumor-associated human carbonic anhydrases (hCA) as promising
therapeutic targets has urged rigorous research into the development of potent and selective …