Synthesis and preliminary anticancer evaluation of new triazole bisphosphonate-based isoprenoid biosynthesis inhibitors.
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Diphosphonates
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Docking Simulation
Molecular Structure
Structure-Activity Relationship
Terpenes
/ antagonists & inhibitors
Triazoles
/ chemical synthesis
Tumor Cells, Cultured
1-Hydroxymethylene-1,1-bisphosphonic acid
Cancer
Chemotherapy
Click chemistry
Mevalonate pathway inhibition
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 2021
15 Mar 2021
Historique:
received:
21
12
2020
revised:
25
01
2021
accepted:
25
01
2021
pubmed:
12
2
2021
medline:
1
5
2021
entrez:
11
2
2021
Statut:
ppublish
Résumé
The synthesis of a new set of triazole bisphosphonates 8a-d and 9a-d presenting an alkyl or phenyl substituent at the C-4 or C-5 position of the triazole ring is described. These compounds have been evaluated for their antiproliferative activity against MIA PaCa-2 (pancreas), MDA-MB-231 (breast) and A549 (lung) human tumor cell lines. 4-hexyl- and 4-octyltriazole bisphosphonates 8b-c both displayed remarkable antiproliferative activities with IC
Identifiants
pubmed: 33571830
pii: S0223-5234(21)00090-8
doi: 10.1016/j.ejmech.2021.113241
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Diphosphonates
0
Terpenes
0
Triazoles
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
113241Informations de copyright
Copyright © 2021 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.