Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and biological evaluation.

Clicks: 550
ID: 70142
2020
Article Quality & Performance Metrics
Overall Quality
Not rated
Combines reader engagement with the AI quality analysis. This article has not been analysed, so there is no overall score — reader engagement is measured and shown alongside.
AI Quality Assessment
Not analyzed
Readership in this journal
Emerging

Ranked #2 of 403 articles by views in Journal of enzyme inhibition and medicinal chemistry

Most read Least read

Bar heights use a square-root scale. Only the 120 most-read articles are drawn; the journal has 403 in total.

Mint this article as an NFT
Not yet minted

Create a permanent, verifiable on-chain record of this article on the Scimatic Network. The NFT is held in your Journament account, and you can withdraw it to your own wallet at any time.

5 SUSD one-off · no wallet required
Sign in to mint
Abstract
Pursuing on our efforts toward searching for efficient hCA IX and hCA XII inhibitors, herein we report the design and synthesis of new sets of benzofuran-based sulphonamides (,, ,, , and ), featuring the zinc anchoring benzenesulfonamide moiety linked to a benzofuran tail a hydrazine or hydrazide linker. All the target benzofurans were examined for their inhibitory activities toward isoforms hCA I, II, IX, and XII. The target tumour-associated hCA IX and XII isoforms were efficiently inhibited with s spanning in ranges 10.0-97.5 and 10.1-71.8 nM, respectively. Interestingly, arylsulfonehydrazones displayed the best selectivity toward hCA IX and XII over hCA I (SIs: 39.4-250.3 and 26.0-149.9, respectively), and over hCA II (SIs: 19.6-57.1 and 13.0-34.2, respectively). Furthermore, the target benzofurans were assessed for their anti-proliferative activity, according to US-NCI protocol, toward a panel of sixty cancer cell lines. Only benzofurans and possessed selective and moderate growth inhibitory activity toward certain cancer cell lines.
Reference Key
abdelrahman2020noveljournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Abdelrahman, Mohamed A;Eldehna, Wagdy M;Nocentini, Alessio;Ibrahim, Hany S;Almahli, Hadia;Abdel-Aziz, Hatem A;Abou-Seri, Sahar M;Supuran, Claudiu T;
Journal Journal of enzyme inhibition and medicinal chemistry
Year 2020
DOI
10.1080/14756366.2019.1697250
URL
Keywords
synthesis anticancer benzenesulfonamides benzofurans carbonic anhydrases

Citations

No citations found. To add a citation, contact the admin at info@scimatic.org

Comments

No comments yet. Be the first to comment on this article.