Synthesis of 5-enamine-4-thiazolidinone derivatives with trypanocidal and anticancer activity.
Animals
Antiprotozoal Agents
/ chemical synthesis
Cell Line
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Parasitic Sensitivity Tests
Rats
Structure-Activity Relationship
Thiazolidines
/ chemical synthesis
Trypanocidal Agents
/ chemical synthesis
Trypanosoma brucei brucei
/ drug effects
5-ene-4-thiazolidinones
Anticancer activity
Antitrypanosomal activity
X-ray
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
05 2019
05 2019
Historique:
received:
19
11
2018
revised:
20
12
2018
accepted:
20
01
2019
pubmed:
29
1
2019
medline:
1
4
2020
entrez:
29
1
2019
Statut:
ppublish
Résumé
A series of novel 2-(5-aminomethylene-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropionic acid ethyl esters has been synthesized. Target compounds were evaluated for their trypanocidal activity towards Trypanosoma brucei brucei and Trypanosoma brucei gambiense. Several hit-compounds (8, 10, 12) inhibited growth of the parasites at sub-micromolar concentrations (IC
Identifiants
pubmed: 30690336
pii: S0045-2068(18)31353-1
doi: 10.1016/j.bioorg.2019.01.045
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Thiazolidines
0
Trypanocidal Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
126-136Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.