New bioactive 5-arylcarboximidamidopyrazolo[3,4-c]pyridines: Synthesis, cytotoxic activity, mechanistic investigation and structure-activity relationships.
Akt
Apoptosis
Cell cycle analysis
Cytotoxicity
ERK
Purine analogues
Pyrazolopyridine
p38 MAPK
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:
05 Jun 2021
05 Jun 2021
Historique:
received:
10
01
2021
revised:
11
03
2021
accepted:
14
03
2021
pubmed:
29
3
2021
medline:
7
8
2021
entrez:
28
3
2021
Statut:
ppublish
Résumé
In this study, a series of novel substituted pyrazolo[3,4-c]pyridin-5-ylamidines was synthesized and their cytotoxicity against three cancer cell lines (MDA-MB-231, HT-1080, PC-3), as well as a human normal cell line (AG01523) was evaluated. A number of derivatives could strongly reduce cancer cells proliferation and exhibit apoptotic induction capability, while reasonable structure-activity relationships could be extracted. Certain analogues were endowed with low toxicity against normal cells. Cell cycle analysis revealed that most of the active compounds induced a G
Identifiants
pubmed: 33774342
pii: S0223-5234(21)00236-1
doi: 10.1016/j.ejmech.2021.113387
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
113387Informations 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 conflict of interest to disclosure.