Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies

M Kciuk, A Gielecińska, S Mujwar… - Journal of Enzyme …, 2022 - Taylor & Francis
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 …

Anticancer therapeutic potential of benzofuran scaffolds

AA Abbas, KM Dawood - RSC advances, 2023 - pubs.rsc.org
Benzofuran moiety is the main component of many biologically active natural and synthetic
heterocycles. These heterocycles have unique therapeutic potentials and are involved in …

A decade of tail-approach based design of selective as well as potent tumor associated carbonic anhydrase inhibitors

A Kumar, K Siwach, CT Supuran, PK Sharma - Bioorganic Chemistry, 2022 - Elsevier
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 …

Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail …

HO Tawfik, A Petreni, CT Supuran… - European journal of …, 2022 - Elsevier
The hydrophobic and the hydrophilic rims in the active site of human carbonic anhydrase IX
(hCA IX) which as well contains a zinc ion as part of the catalytic core, were simultaneously …

From antibacterial to antitumour agents: a brief review on the chemical and medicinal aspects of sulfonamides

H Azevedo-Barbosa, DF Dias, LL Franco… - Mini Reviews in …, 2020 - ingentaconnect.com
Sulfonamides have been in clinical use for many years, and the development of bioactive
substances containing the sulfonamide subunit has grown steadily in view of their important …

Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors

M Shaldam, WM Eldehna, A Nocentini… - European Journal of …, 2021 - Elsevier
In the present study, we describe the design of different series of benzofuran-based
derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based …

Discovery of 2, 4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms

WM Eldehna, MS Taghour, T Al-Warhi… - Journal of Enzyme …, 2022 - Taylor & Francis
Abstract Different 2, 4-thiazolidinedione-tethered coumarins 5a–b, 10a–n and 11a–d were
synthesised and evaluated for their inhibitory action against the cancer-associated h CAs IX …

Benzofuran-based carboxylic acids as carbonic anhydrase inhibitors and antiproliferative agents against breast cancer

WM Eldehna, A Nocentini, ZM Elsayed… - ACS Medicinal …, 2020 - ACS Publications
Pursuing our effort for developing effective inhibitors of the cancer-related hCA IX isoform,
here we describe the synthesis of novel benzofuran-based carboxylic acid derivatives …

Insights into the effect of elaborating coumarin-based aryl enaminones with sulfonamide or carboxylic acid functionality on carbonic anhydrase inhibitory potency and …

HS Ibrahim, MA Abdelrahman, A Nocentini, S Bua… - Bioorganic …, 2022 - Elsevier
Recently, different mechanisms for inhibition of carbonic anhydrases (CAs) have been
reported, such as the classical zinc-binding (exerted by sulfonamides and carboxylic acids) …

Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors

DM Elimam, WM Eldehna, R Salem, A Bonardi… - European Journal of …, 2022 - Elsevier
Ligustrazine is the principle bioactive alkaloid in the widely-used Chinese herb Chuan
Xiong rhizome. Herein, a series of novel derivatives has been designed as human carbonic …