Novel beta-lactam substituted benzenesulfonamides: in vitro enzyme inhibition, cytotoxic activity and in silico interactions

Ö Güleç, C Türkeş, M Arslan, Y Demir… - Journal of …, 2023 - Taylor & Francis
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 …

PET radiotracers and fluorescent probes for imaging human carbonic anhydrase IX and XII in hypoxic tumors

SG Nerella, P Singh, PS Thacker, M Arifuddin… - Bioorganic …, 2023 - Elsevier
Positron emission tomography (PET) and fluorescent imaging play a pivotal role in medical
diagnosis, biomedical oncologic research, and drug development process, which include …

Discovery of sulfonamide-tethered isatin derivatives as novel anticancer agents and VEGFR-2 inhibitors

MA Shaldam, H Almahli, A Angeli, RM Badi… - Journal of Enzyme …, 2023 - Taylor & Francis
In this work, new isatin-based sulphonamides (6a-i, 11a-c, 12a-c) were designed and
synthesised as potential dual VEGFR-2 and carbonic anhydrase inhibitors with anticancer …

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 …

Design and synthesis of 6-arylpyridine-tethered sulfonamides as novel selective inhibitors of carbonic anhydrase IX with promising antitumor features toward the …

WM Eldehna, EE Mohammed, GH Al-Ansary… - European Journal of …, 2023 - Elsevier
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 …

Terminators or guardians? design, synthesis, and cytotoxicity profiling of chalcone-sulfonamide hybrids

SM Aboukhatwa, PA Sidhom, A Angeli, CT Supuran… - ACS …, 2023 - ACS Publications
With a “less is more” philosophy, a series of 15 chalcone-sulfonamide hybrids were
designed anticipating synergistic anticancer activity. The aromatic sulfonamide moiety was …

Benzenesulfonamides with different rigidity-conferring linkers as carbonic anhydrase inhibitors: an insight into the antiproliferative effect on glioblastoma, pancreatic …

F Liguori, S Carradori, R Ronca, S Rezzola… - Journal of Enzyme …, 2022 - Taylor & Francis
Among the chemotypes studied for selective inhibition of tumour-associated carbonic
anhydrases (CAs), SLC-0111, a ureido-bearing benzenesulfonamide CA IX inhibitor …

4-(3-Alkyl/benzyl-guanidino) benzenesulfonamides as selective carbonic anhydrase VII inhibitors

M Abdoli, S Giovannuzzi, CT Supuran… - Journal of Enzyme …, 2022 - Taylor & Francis
The treatment of chronic neuropathic pain remains one of the most challenging of all
neurological diseases and very much an art. There exists no consensus for the optimal …

Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In …

SM Hefny, TF El-Moselhy, N El-Din… - Journal of Medicinal …, 2024 - ACS Publications
A dual-targeting approach is predicted to yield better cancer therapy outcomes.
Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed and …

Dependence on linkers' flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents

HO Tawfik, A Belal, MAS Abourehab… - Journal of Enzyme …, 2022 - Taylor & Francis
Herein we reported the design and synthesis of two series comprising twenty-two
benzenesulfonamides that integrate the s-triazine moiety. Target compounds successfully …