Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 3, Pages 313-317Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500496u
Keywords
Dasatinib; medicinal chemistry; angiogenesis; antiangiogenic drugs; kinase inhibitors
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Funding
- Swiss National Science Foundation
- EPFL
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Dasatinib is an orally active nonselective tyrosine kinase inhibitor used to treat certain types of adult leukemia. By inhibiting PDGFR-beta and SFKs in both tumor cells and tumor associated endothelial cells, dasatinib inhibits tumor growth and angiogenesis. Herein, dasatinib derivatives modified with hydrophobic chains were prepared and evaluated for their in vitro antiproliferative selectivity and their in vivo antiangiogenic activity. For one of the derivatives, modified with a long perfluorinated chain, a significant enhancement in antiangiogenic activity was observed. Combined, these results suggest a possible generic route to modulate the angiostatic activity of drugs.
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