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 …
2-Aminobenzothiazoles in anticancer drug design and discovery
G Huang, T Cierpicki, J Grembecka - Bioorganic chemistry, 2023 - Elsevier
Cancer is one of the major causes of mortality and morbidity worldwide. Substantial
research efforts have been made to develop new chemical entities with improved anticancer …
research efforts have been made to develop new chemical entities with improved anticancer …
Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro …
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
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) …
4-(5-Amino-pyrazol-1-yl) benzenesulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and …
In the current medical era, the single target inhibition paradigm of drug discovery has given
way to the multi-target design concept. As the most intricate pathological process …
way to the multi-target design concept. As the most intricate pathological process …
[HTML][HTML] Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis …
SM Al-Muntaser, AA Al-Karmalawy, AM El-Naggar… - RSC …, 2023 - pubs.rsc.org
In this article, we continued our previous effort to develop new selective anticancer
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …
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 …
Design and synthesis of novel quinazolinone–chalcone hybrids as potential apoptotic candidates targeting caspase-3 and PARP-1: in vitro, molecular docking, and …
EA Madbouly, ESM Lashine, AA Al-Karmalawy… - New Journal of …, 2022 - pubs.rsc.org
A new series of thirty-one quinazolinone–chalcone hybrid molecules 13–43 were designed,
synthesized, and structurally characterized by different spectroscopic techniques. All the …
synthesized, and structurally characterized by different spectroscopic techniques. All the …
Design and synthesis of 6-arylpyridine-tethered sulfonamides as novel selective inhibitors of carbonic anhydrase IX with promising antitumor features toward the …
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 …
proliferation and rapid tumor growth exceeding the oxygen supply, and can result in …
Atropo/Tropo flexibility: a tool for design and synthesis of self-adaptable inhibitors of carbonic anhydrases and their antiproliferative effect
J Ivanova, A Nocentini, K Tars, J Leita̅ns… - Journal of Medicinal …, 2023 - ACS Publications
Here, we report for the first time a series of sulfonamide derivatives with scaffolds bearing
flexible moieties, namely, rotamers or tropoisomers capable of adapting their geometry in …
flexible moieties, namely, rotamers or tropoisomers capable of adapting their geometry in …