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 …
are connected with tumorigenesis. Hypoxic tumors overexpress CA IX and XII as a …
Novel beta-lactam substituted benzenesulfonamides: in vitro enzyme inhibition, cytotoxic activity and in silico interactions
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 …
synthesized using the tail-approach method. The compounds were characterized using IR …
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 …
Discovery of novel pyridazine-tethered sulfonamides as carbonic anhydrase II inhibitors for the management of glaucoma
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …
New acetamide-sulfonamide-containing scaffolds: antiurease activity screening, structure-activity relationship, kinetics mechanism, molecular docking, and md …
The development of novel scaffolds that can increase the effectiveness, safety, and
convenience of medication therapy using drug conjugates is a promising strategy. As a …
convenience of medication therapy using drug conjugates is a promising strategy. As a …
Tail-approach-based design and synthesis of coumarin-monoterpenes as carbonic anhydrase inhibitors and anticancer agents
In this study, sixty novel coumarin-monoterpene compounds were synthesized in two series
[thirty-two compounds (12–43) bearing a triazole ring in the first series, and twenty-eight …
[thirty-two compounds (12–43) bearing a triazole ring in the first series, and twenty-eight …
Exploring the Potential of New Benzamide-Acetamide Pharmacophore Containing Sulfonamide as Urease Inhibitors: Structure–Activity Relationship, Kinetics …
The search for novel drug scaffolds that can improve effectiveness and safety through drug
conjugates is a promising approach. Consequently, drug conjugates constitute a dynamic …
conjugates is a promising approach. Consequently, drug conjugates constitute a dynamic …
Electrophilic hydrazination of cyclopropanols using azodicarboxylates via copper (II) catalysis: an Umpolung strategy to access β-hydrazino ketone motifs
T Ramar, A Ilangovan, NA Meanwell… - The Journal of …, 2022 - ACS Publications
The scope of an umpolung approach to expand synthetic access to bifunctional γ-keto
hydrazine intermediates via electrophilic amination of β-homoenolates derived from …
hydrazine intermediates via electrophilic amination of β-homoenolates derived from …