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 …
are presented, with an emphasis on the deciphering of the activation mechanism, the …
Carbonic anhydrase inhibitors targeting metabolism and tumor microenvironment
The tumor microenvironment is crucial for the growth of cancer cells, triggering particular
biochemical and physiological changes, which frequently influence the outcome of …
biochemical and physiological changes, which frequently influence the outcome of …
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors
Abstract Carbonic anhydrase (CA, EC 4.2. 1.1) is an enzyme and a very omnipresent zinc
metalloenzyme which catalyzed the reversible hydration and dehydration of carbon dioxide …
metalloenzyme which catalyzed the reversible hydration and dehydration of carbon dioxide …
Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase
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 …
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
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 …
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 …
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
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) …
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
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 …
carboxylic acids 14a-c were developed as novel SLC-0111 analogues with the goal of …
Discovery of indolinone-bearing benzenesulfonamides as new dual carbonic anhydrase and VEGFR-2 inhibitors possessing anticancer and pro-apoptotic properties
In the current medical era, the utilization of a single small molecule to simultaneously target
two distinct molecular targets is emerging as a highly effective strategy in the battle against …
two distinct molecular targets is emerging as a highly effective strategy in the battle against …
3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and …
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 …
unsubstituted (4a-c) or N-substituted (7a-o) isatin moieties (as tails) connected to …