Identification of Benzothiazoles Bearing 1,3,4-Thiadiazole as Antiproliferative Hybrids Targeting VEGFR-2 and BRAF Kinase: Design, Synthesis, BIO Evaluation and In Silico Study.
Vascular Endothelial Growth Factor Receptor-2
/ antagonists & inhibitors
Humans
Proto-Oncogene Proteins B-raf
/ antagonists & inhibitors
Protein Kinase Inhibitors
/ pharmacology
Benzothiazoles
/ chemistry
Thiadiazoles
/ chemistry
Cell Line, Tumor
Cell Proliferation
/ drug effects
Antineoplastic Agents
/ pharmacology
Molecular Docking Simulation
Drug Design
Structure-Activity Relationship
Sorafenib
/ pharmacology
Molecular Structure
Computer Simulation
Drug Screening Assays, Antitumor
BRAF inhibition
VEGFR-2 inhibition
antitumor activity
apoptosis
benzothiazoles
cell cycle analysis
molecular docking
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
04 Jul 2024
04 Jul 2024
Historique:
received:
07
06
2024
revised:
29
06
2024
accepted:
01
07
2024
medline:
13
7
2024
pubmed:
13
7
2024
entrez:
13
7
2024
Statut:
epublish
Résumé
Cancer remains a leading cause of death worldwide, often resulting from uncontrolled growth in various organs. Protein kinase inhibitors represent an important class of targeted cancer therapies. Recently, the kinases BRAF and VEGFR-2 have shown synergistic effects on tumor progression. Seeking to develop dual BRAF/VEGFR-2 inhibitors, we synthesized 18 amino-benzothiazole derivatives with structural similarities to reported dual inhibitors. Four compounds-
Identifiants
pubmed: 38999138
pii: molecules29133186
doi: 10.3390/molecules29133186
pii:
doi:
Substances chimiques
Vascular Endothelial Growth Factor Receptor-2
EC 2.7.10.1
Proto-Oncogene Proteins B-raf
EC 2.7.11.1
Protein Kinase Inhibitors
0
Benzothiazoles
0
Thiadiazoles
0
Antineoplastic Agents
0
1,3,4-thiadiazole
14IAC3GH7G
BRAF protein, human
EC 2.7.11.1
KDR protein, human
EC 2.7.10.1
Sorafenib
9ZOQ3TZI87
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : King Saud University, Riyadh, Saudi Arabia.
ID : Research supporting project number (RSPD2024R740)