Synthesis, evaluation of thymidine phosphorylase and angiogenic inhibitory potential of ciprofloxacin analogues: Repositioning of ciprofloxacin from antibiotic to future anticancer drugs.
Angiogenesis Inhibitors
/ chemical synthesis
Animals
Anti-Bacterial Agents
/ chemical synthesis
Antineoplastic Agents
/ chemical synthesis
Chick Embryo
Ciprofloxacin
/ analogs & derivatives
Drug Repositioning
Enzyme Inhibitors
/ chemical synthesis
Humans
Molecular Docking Simulation
Thymidine Phosphorylase
/ antagonists & inhibitors
Antiangiogenic activity
Ciprofloxacin
Thymidine phosphorylase inhibitors
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
07 2020
07 2020
Historique:
received:
13
02
2020
revised:
07
04
2020
accepted:
21
04
2020
pubmed:
11
5
2020
medline:
9
3
2021
entrez:
11
5
2020
Statut:
ppublish
Résumé
Over expression of thymidine phosphorylase (TP) in various human tumors compared to normal healthy tissue is associated with progression of cancer and proliferation. The 2-deoxy-d-ribose is the final product of thymidine phosphorylase (TP) catalyzed reaction. Both TP and 2-deoxy-d-ribose are known to promote unwanted angiogenesis in cancerous cells. Discovery of potent inhibitors of thymidine phosphorylase (TP) can offer appropriate approach in cancer treatment. A series of ciprofloxacin 2, 3a-3c, 4a-4d, 5a-5b, 6 and 7 has been synthesized and characterized using spectroscopic techniques. Afterwards, inhibitory potential of synthesized ciprofloxacin 2, 3a-3c, 4a-4d, 5a-5b, 6 and 7 against thymidine phosphorylase enzyme was assessed. Out of these twelve analogs of ciprofloxacin nine analogues 3a-3c, 4a-4c, 5a-5b and 6 showed good inhibitory activity against thymidine phosphorylase. Inhibitory activity as presented by their IC
Identifiants
pubmed: 32388426
pii: S0045-2068(20)30360-6
doi: 10.1016/j.bioorg.2020.103876
pii:
doi:
Substances chimiques
Angiogenesis Inhibitors
0
Anti-Bacterial Agents
0
Antineoplastic Agents
0
Enzyme Inhibitors
0
Ciprofloxacin
5E8K9I0O4U
Thymidine Phosphorylase
EC 2.4.2.4
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103876Informations de copyright
Copyright © 2020 Elsevier Inc. 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.