Back to Search
Start Over
Discovery of new VEGFR-2 inhibitors and apoptosis inducer-based thieno[2,3- d ]pyrimidine.
- Source :
-
Future medicinal chemistry [Future Med Chem] 2023 Nov; Vol. 15 (22), pp. 2065-2086. Date of Electronic Publication: 2023 Nov 13. - Publication Year :
- 2023
-
Abstract
- Background: VEGFR-2 is a key regulator of cancer cell proliferation, migration and angiogenesis. Aim: Development of thieno[2,3- d ]pyrimidine derivatives as potential anti-cancer agents targeting VEGFR-2. Methods: Seven in vitro and nine in silico studies were conducted. Results: Compound 10d demonstrated strong anticancer potential, boosting apoptosis based on VEGFR-2 inhibition. It arrested the S phase of the cell cycle and upregulated the apoptotic factors. Docking and molecular dynamics simulation studies confirm the stability of the VEGFR-2- 10d complex and suggest that these compounds have good binding affinities to VEGFR-2. In addition, the drug-likeness was confirmed. Conclusion: Thieno[2,3- d ]pyrimidines, particularly compound 10d , has good anticancer effects and may contribute to the development of new anticancer therapies.
Details
- Language :
- English
- ISSN :
- 1756-8927
- Volume :
- 15
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Future medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 37955128
- Full Text :
- https://doi.org/10.4155/fmc-2023-0130