Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors.
1,3]thiazolo[4,5-e]isoindoles
Apoptosis
Cell cycle arrest
Tubulin polymerization inhibitors
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 Feb 2021
15 Feb 2021
Historique:
received:
13
11
2020
revised:
15
12
2020
accepted:
18
12
2020
pubmed:
6
1
2021
medline:
24
4
2021
entrez:
5
1
2021
Statut:
ppublish
Résumé
A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs.
Identifiants
pubmed: 33401199
pii: S0223-5234(20)31094-1
doi: 10.1016/j.ejmech.2020.113122
pii:
doi:
Substances chimiques
Isoindoles
0
Tubulin
0
Tubulin Modulators
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
113122Informations 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.