Synthesis and biological evaluation of quinoxaline derivatives as tubulin polymerization inhibitors that elevate intracellular ROS and triggers apoptosis via mitochondrial pathway.
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Binding Sites
Cell Line, Tumor
Cyclin-Dependent Kinase Inhibitor p21
/ metabolism
Dose-Response Relationship, Drug
G2 Phase Cell Cycle Checkpoints
/ drug effects
Humans
Membrane Potential, Mitochondrial
/ drug effects
Mitochondria
/ drug effects
Molecular Docking Simulation
Protein Structure, Tertiary
Quinoxalines
/ chemistry
Reactive Oxygen Species
/ metabolism
Structure-Activity Relationship
Tubulin
/ chemistry
Tubulin Modulators
/ chemical synthesis
Up-Regulation
/ drug effects
G2/M phase arrest
cell apoptosis
quinoxaline derivatives
reactive oxygen species
tubulin polymerization inhibitors
Journal
Chemical biology & drug design
ISSN: 1747-0285
Titre abrégé: Chem Biol Drug Des
Pays: England
ID NLM: 101262549
Informations de publication
Date de publication:
04 2019
04 2019
Historique:
received:
11
07
2018
revised:
19
11
2018
accepted:
24
11
2018
pubmed:
13
1
2019
medline:
16
1
2020
entrez:
13
1
2019
Statut:
ppublish
Résumé
A series of novel quinoxaline derivatives were synthesized and evaluated for their antiproliferative activity in three human cancer cell lines. Compound 12 exhibited the most potent antiproliferative activity with IC
Substances chimiques
Antineoplastic Agents
0
Cyclin-Dependent Kinase Inhibitor p21
0
Quinoxalines
0
Reactive Oxygen Species
0
Tubulin
0
Tubulin Modulators
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
617-627Informations de copyright
© 2019 John Wiley & Sons A/S.