Systematic Studies on Anti-Cancer Evaluation of Stilbene and Dibenzo[
biological activity
cancer cell
colchicine-binding site
dibenzo[b,f]oxepine
microtubule
tubulin
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
18 Apr 2023
18 Apr 2023
Historique:
received:
06
03
2023
revised:
13
04
2023
accepted:
14
04
2023
medline:
1
5
2023
pubmed:
28
4
2023
entrez:
28
4
2023
Statut:
epublish
Résumé
Cancer is one of the most common causes of human death worldwide; thus, numerous therapies, including chemotherapy, have been and are being continuously developed. In cancer cells, an aberrant mitotic spindle-a microtubule-based structure necessary for the equal splitting of genetic material between daughter cells-leads to genetic instability, one of the hallmarks of cancer. Thus, the building block of microtubules, tubulin, which is a heterodimer formed from α- and β-tubulin proteins, is a useful target in anti-cancer research. The surface of tubulin forms several pockets, i.e., sites that can bind factors that affect microtubules' stability. Colchicine pockets accommodate agents that induce microtubule depolymerization and, in contrast to factors that bind to other tubulin pockets, overcome multi-drug resistance. Therefore, colchicine-pocket-binding agents are of interest as anti-cancer drugs. Among the various colchicine-site-binding compounds, stilbenoids and their derivatives have been extensively studied. Herein, we report systematic studies on the antiproliferative activity of selected stilbenes and oxepine derivatives against two cancer cell lines-HCT116 and MCF-7-and two normal cell lines-HEK293 and HDF-A. The results of molecular modeling, antiproliferative activity, and immunofluorescence analyses revealed that compounds
Identifiants
pubmed: 37110792
pii: molecules28083558
doi: 10.3390/molecules28083558
pmc: PMC10146957
pii:
doi:
Substances chimiques
Tubulin
0
Stilbenes
0
Oxepins
0
Antineoplastic Agents
0
Colchicine
SML2Y3J35T
Tubulin Modulators
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Warsaw University of Technology
ID : Research University (IDUB) program (NChem 3)
Organisme : National Science Center
ID : OPUS15 2018/29/B/NZ3/02443
Organisme : Operational Project Knowledge Education Development 2014-2020 co-financed by the European Social Fund
ID : POWR.03.02.00-00-I007/16-00 (POWER 2014-2020)
Organisme : budget funds for science in the years 2019-2023
ID : Diamond Grant project
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