Inclusion of a 5-fluorouracil moiety in nitrogenous bases derivatives as human carbonic anhydrase IX and XII inhibitors produced a targeted action against MDA-MB-231 and T47D breast cancer cells.
Antigens, Neoplasm
/ chemistry
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Carbonic Anhydrase IX
/ antagonists & inhibitors
Carbonic Anhydrase Inhibitors
/ chemical synthesis
Carbonic Anhydrases
/ chemistry
Catalytic Domain
Cell Line, Tumor
Coumarins
/ chemical synthesis
Crystallography, X-Ray
Drug Design
Drug Screening Assays, Antitumor
Fluorouracil
/ analogs & derivatives
G2 Phase Cell Cycle Checkpoints
/ drug effects
Humans
Molecular Structure
Protein Binding
Structure-Activity Relationship
Sulfonamides
/ chemical synthesis
5-Fluorouracil
Annexin
Anticancer
Breast cancer
Carbonic anhydrase
Selectivity
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Mar 2020
15 Mar 2020
Historique:
received:
15
01
2020
revised:
31
01
2020
accepted:
31
01
2020
pubmed:
12
2
2020
medline:
15
12
2020
entrez:
12
2
2020
Statut:
ppublish
Résumé
A new series of pyrimidine derivatives as human carbonic anhydrases (CA, EC 4.2.1.1) inhibitors is here designed by including a 5-fluorouracil (5-FU) moiety, broadly used anticancer medication, in nitrogenous base modulators of the tumor-associated CAs. Most sulfonamide derivatives efficiently inhibit the target CA IX (K
Identifiants
pubmed: 32044580
pii: S0223-5234(20)30079-9
doi: 10.1016/j.ejmech.2020.112112
pii:
doi:
Substances chimiques
Antigens, Neoplasm
0
Antineoplastic Agents
0
Carbonic Anhydrase Inhibitors
0
Coumarins
0
Sulfonamides
0
CA9 protein, human
EC 4.2.1.1
Carbonic Anhydrase IX
EC 4.2.1.1
Carbonic Anhydrases
EC 4.2.1.1
carbonic anhydrase XII
EC 4.2.1.1
Fluorouracil
U3P01618RT
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112112Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.