Synthesis and Biological Evaluation of Small Molecules as Potential Anticancer Multitarget Agents.
Antineoplastic Agents
B7-H1 Antigen
Cell Line, Tumor
Cell Proliferation
Drug Screening Assays, Antitumor
HEK293 Cells
Humans
Molecular Docking Simulation
Proto-Oncogene Proteins c-myc
/ metabolism
Structure-Activity Relationship
Triazoles
/ pharmacology
Vascular Endothelial Growth Factor A
/ pharmacology
Vascular Endothelial Growth Factor Receptor-2
/ metabolism
PD-L1
VEGFR-2
angiogenesis
c-Myc
flow cytometry
immunomodulation
multitarget inhibitors
non-peptidic small molecules
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
24 Jun 2022
24 Jun 2022
Historique:
received:
24
04
2022
revised:
20
06
2022
accepted:
21
06
2022
entrez:
9
7
2022
pubmed:
10
7
2022
medline:
14
7
2022
Statut:
epublish
Résumé
Twenty-six triazole-based derivatives were designed for targeting both PD-L1 (programmed death receptor ligand 1) and VEGFR-2 (vascular endothelial growth factor receptor 2). These compounds were synthetized and biologically evaluated as multitarget inhibitors of VEGFR-2, PD-L1 and c-Myc proteins. The antiproliferative activity of these molecules on several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was determined. The effects on the abovementioned biological targets were evaluated for some selected compounds. Compound
Identifiants
pubmed: 35806053
pii: ijms23137049
doi: 10.3390/ijms23137049
pmc: PMC9266368
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
B7-H1 Antigen
0
Proto-Oncogene Proteins c-myc
0
Triazoles
0
Vascular Endothelial Growth Factor A
0
Vascular Endothelial Growth Factor Receptor-2
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Universitat Jaume I
ID : projects UJI-B2018-38 and UJI-B2019-43
Organisme : Ministerio de Economía y Competitividad
ID : project RTI2018-097345-B-I00
Organisme : Generalitat Valenciana
ID : ACIF/2020/341
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