| Autor: |
Mannion M; Department of Medicinal Chemistry, MethylGene Inc, Montréal, QC, Canada., Raeppel S, Claridge S, Zhou N, Saavedra O, Isakovic L, Zhan L, Gaudette F, Raeppel F, Déziel R, Beaulieu N, Nguyen H, Chute I, Beaulieu C, Dupont I, Robert MF, Lefebvre S, Dubay M, Rahil J, Wang J, Ste-Croix H, Robert Macleod A, Besterman JM, Vaisburg A |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Dec 01; Vol. 19 (23), pp. 6552-6. Date of Electronic Publication: 2009 Oct 13. |
| DOI: |
10.1016/j.bmcl.2009.10.040 |
| Abstrakt: |
A series of N-(4-(6,7-disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC(50) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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