Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: Where are we today?
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 …
both prokaryotes and eukaryotes. They efficiently catalyze the reversible hydration of carbon …
Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies
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 …
that catalyze a very basic but crucial physiological reaction: the conversion of carbon dioxide …
Exploration of 1, 2, 3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase
Abstract A novel series of 1, 2, 3-triazole benzenesulfonamide substituted 1, 3-
dioxoisoindolin-5-carboxylate (7a-l) inhibitors of human α-carbonic anhydrase (hCA) was …
dioxoisoindolin-5-carboxylate (7a-l) inhibitors of human α-carbonic anhydrase (hCA) was …
Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008–2018)
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 …
proteins, being part of the molecular machinery that tumor cells build as adaptive responses …
A decade of tail-approach based design of selective as well as potent tumor associated carbonic anhydrase inhibitors
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 …
anticancer drug targets and their selective inhibition is highly desired for the proper …
Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted …
Herein we report the design and synthesis of novel N-substituted isatins-SLC-0111 hybrids
(6a-f and 9a-l). A structural extension approach was adopted via N-alkylation and N …
(6a-f and 9a-l). A structural extension approach was adopted via N-alkylation and N …
Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine–Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors
HT Abdel-Mohsen, AM El Kerdawy, MA Omar… - European Journal of …, 2022 - Elsevier
A dual-tail approach was applied to the design of a novel series of 2-thiopyrimidine–
benzenesulfonamides as carbonic anhydrase (CA) inhibitors. The design strategy is based …
benzenesulfonamides as carbonic anhydrase (CA) inhibitors. The design strategy is based …
Multiple Binding Modes of Inhibitors to Human Carbonic Anhydrases: An Update on the Design of Isoform-Specific Modulators of Activity
K D'Ambrosio, A Di Fiore, V Alterio, E Langella… - Chemical …, 2024 - ACS Publications
Human carbonic anhydrases (hCAs) are widespread zinc enzymes that catalyze the
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …
Drug screening in human cells by NMR spectroscopy allows the early assessment of drug potency
Abstract Structure‐based drug development is often hampered by the lack of in vivo activity
of promising compounds screened in vitro, due to low membrane permeability or poor …
of promising compounds screened in vitro, due to low membrane permeability or poor …
Erlotinib-Containing Benzenesulfonamides As Anti-Helicobacter Pylori Agents Through Carbonic Anhydrase Inhibition
G Benito, I D'Agostino, S Carradori… - Future Medicinal …, 2023 - Taylor & Francis
Aim: Development of dual-acting antibacterial agents containing Erlotinib, a recognized
EGFR inhibitor used as an anticancer agent, with differently spaced benzenesulfonamide …
EGFR inhibitor used as an anticancer agent, with differently spaced benzenesulfonamide …