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Page 1
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H. Barrett SD, et al. Among authors: leopold wr. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. Bioorg Med Chem Lett. 2008. PMID: 18952427
2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).
Warmus JS, Flamme C, Zhang LY, Barrett S, Bridges A, Chen H, Gowan R, Kaufman M, Sebolt-Leopold J, Leopold W, Merriman R, Ohren J, Pavlovsky A, Przybranowski S, Tecle H, Valik H, Whitehead C, Zhang E. Warmus JS, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6171-4. doi: 10.1016/j.bmcl.2008.10.015. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18951019
C-terminal modifications of histidyl-N-benzylglycinamides to give improved inhibition of Ras farnesyltransferase, cellular activity, and anticancer activity in mice.
McNamara DJ, Dobrusin E, Leonard DM, Shuler KR, Kaltenbronn JS, Quin J 3rd, Bur S, Thomas CE, Doherty AM, Scholten JD, Zimmerman KK, Gibbs BS, Gowan RC, Latash MP, Leopold WR, Przybranowski SA, Sebolt-Leopold JS. McNamara DJ, et al. Among authors: leopold wr. J Med Chem. 1997 Oct 10;40(21):3319-22. doi: 10.1021/jm970470c. J Med Chem. 1997. PMID: 9341905 No abstract available.
Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo.
Sebolt-Leopold JS, Dudley DT, Herrera R, Van Becelaere K, Wiland A, Gowan RC, Tecle H, Barrett SD, Bridges A, Przybranowski S, Leopold WR, Saltiel AR. Sebolt-Leopold JS, et al. Among authors: leopold wr. Nat Med. 1999 Jul;5(7):810-6. doi: 10.1038/10533. Nat Med. 1999. PMID: 10395327
Cellular transport of CI-980.
Hook KE, Przybranowski SA, Leopold WR. Hook KE, et al. Among authors: leopold wr. Invest New Drugs. 1996;14(4):341-7. doi: 10.1007/BF00180809. Invest New Drugs. 1996. PMID: 9157068
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM. Fry DW, et al. Among authors: leopold wr. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. doi: 10.1073/pnas.95.20.12022. Proc Natl Acad Sci U S A. 1998. PMID: 9751783 Free PMC article.
69 results