Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases
Login
MSAR Home
→
MSA University Academic Research
→
Research Papers, Articles and Books Chapters.
→
Faculty Of Pharmacy Research Paper
→
View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.
Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases
Supuran, C.T.
;
Nissan, Y.M
;
El Sayed Teba, H.
;
Bua, S
;
Kamal, A.M
;
Khalil, O.M
Full Text link:
https://t.ly/dNr0z
Date issued:
2/15/2020
Scientific Journal Rankings:
Click Here
Doi:
https://doi.org/10.1016/j.ejmech.2019.112021
Publisher:
Elsevier Masson SAS
Series Info:
European Journal of Medicinal Chemistry;Volume 188, 15 February 2020, Article number 112021
Type:
Article
Keywords:
Sulfonamide , Pyrrolopyrimidine , Cytotoxic , Carbonic anhydrase inhibitor
Abstract:
A series of novel sulfonamide derivatives bearing pyrrole and pyrrolopyrimidine scaffolds were synthesized and screened as carbonic anhydrase inhibitors. The inhibition activity of the synthesized compounds was evaluated against the cytosolic human carbonic anhydrase isoforms I and II and the transmembranal isoforms IX and XII. Several candidates showed potent inhibitory activity against IX and XII isoforms. Furthermore, ex vivo screening of cytotoxic selectivity and activity of the most potent derivatives were carried out against normal cells (WI38) and cervical cancer cell line (HeLa) under normal and hypoxic conditions using acetazolamide as reference drug. Compound 11b potency was nearly three folds higher in hypoxic than normoxic condition whereas that of compound 11f was nearly four folds higher in hypoxic vs. normoxic HeLa cells. All the screened derivatives exhibited less potency on normal cells (WI38). Molecular docking was carried out to discover the possible binding mode of compounds within the active site of isoform CA IX. © 2019 Elsevier Masson SAS
Description:
scopus
Show full item record
Files in this item
Name:
avatar_scholar_128.png
Size:
2.731Kb
Format:
PNG image
View/
Open
This item appears in the following Collection(s)
Faculty Of Pharmacy Research Paper
[1121]
Search MSAR
Search MSAR
This Collection
Advanced Search
Browse
All of DSpace
Communities & Collections
By Issue Date
Authors
Titles
Subjects
This Collection
By Issue Date
Authors
Titles
Subjects
My Account
Login
Register