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 …

Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies

M Kciuk, A Gielecińska, S Mujwar… - Journal of Enzyme …, 2022 - Taylor & Francis
Carbonic anhydrases IX and CAXII (CAIX/CAXII) are transmembrane zinc metalloproteins
that catalyze a very basic but crucial physiological reaction: the conversion of carbon dioxide …

Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular docking studies of new imidazolyl hydrazone derivatives

M Tapera, H Kekeçmuhammed, B Tüzün… - Journal of molecular …, 2022 - Elsevier
A new series of imidazolyl hydrazone derivatives IA (1-12) were prepared from a
condensation reaction between indoline-2, 3-dione (isatin) and 2 …

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 …

Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

RS Keri, S Budagumpi… - Journal of Clinical …, 2022 - Wiley Online Library
What is known and objective The main objective of this review is to highlight the most
relevant studies since 1990 (to date) in the area of medicinal chemistry aspects to provide a …

Carbonic anhydrase inhibitors: an update on experimental agents for the treatment and imaging of hypoxic tumors

CT Supuran - Expert Opinion on Investigational Drugs, 2021 - Taylor & Francis
Introduction Hypoxic tumors, unlike normal tissues, overexpress proteins involved in oxygen
sensing, metabolism, pH regulation, angiogenesis, immunological response, and other …

An update on synthesis of coumarin sulfonamides as enzyme inhibitors and anticancer agents

L Rubab, S Afroz, S Ahmad, S Hussain, I Nawaz… - Molecules, 2022 - mdpi.com
Coumarin is an important six-membered aromatic heterocyclic pharmacophore, widely
distributed in natural products and synthetic molecules. The versatile and unique features of …

pH regulators and their inhibitors in tumor microenvironment

S Liao, G Wu, Z Xie, X Lei, X Yang, S Huang… - European journal of …, 2024 - Elsevier
As an important characteristic of tumor, acidic tumor microenvironment (TME) is closely
related to immune escape, invasion, migration and drug resistance of tumor. The acidity of …

Discovery of 2, 4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms

WM Eldehna, MS Taghour, T Al-Warhi… - Journal of Enzyme …, 2022 - Taylor & Francis
Abstract Different 2, 4-thiazolidinedione-tethered coumarins 5a–b, 10a–n and 11a–d were
synthesised and evaluated for their inhibitory action against the cancer-associated h CAs IX …

Synthesis and biological evaluation of new 3-substituted coumarin derivatives as selective inhibitors of human carbonic anhydrase IX and XII

S Mahammad Ghouse, K Bahatam… - Journal of Enzyme …, 2023 - Taylor & Francis
The Carbonic anhydrase isoforms IX and XII play a significant role in regulating the
intracellular and extracellular pH in hypoxic tumours abetting the metastasis of solid …