Some will have noted that I just added ONXX to "2000".
That brings up the general question....... if Glaxo goes for Bayer, which Bayer collaborations might Glaxo jettison?
Any ideas?
Bioorg Med Chem Lett 2000 Feb 7;10(3):223-6
The discovery of potent cRaf1 kinase inhibitors.
Lackey K, Cory M, Davis R, Frye SV, Harris PA, Hunter RN, Jung DK, McDonald
OB, McNutt RW, Peel MR, Rutkowske RD, Veal JM, Wood ER.
Glaxo Wellcome, Inc., Research Triangle Park, NC 27709, USA.
kel8725@glaxowellcome.com
A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as
cRaf-1 kinase inhibitors. The key features of the molecules were the donor/acceptor motif
common to kinase inhibitors and a critical acidic phenol flanked by two substitutions. Diverse
5-position substitutions provided compounds with low nanomolar kinase enzyme inhibition and
inhibited the intracellular MAPK pathway. |
