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Page 1
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.
Spicer JA, Rewcastle GW, Kaufman MD, Black SL, Plummer MS, Denny WA, Quin J 3rd, Shahripour AB, Barrett SD, Whitehead CE, Milbank JB, Ohren JF, Gowan RC, Omer C, Camp HS, Esmaeil N, Moore K, Sebolt-Leopold JS, Pryzbranowski S, Merriman RL, Ortwine DF, Warmus JS, Flamme CM, Pavlovsky AG, Tecle H. Spicer JA, et al. Among authors: gowan rc. J Med Chem. 2007 Oct 18;50(21):5090-102. doi: 10.1021/jm0704548. Epub 2007 Sep 19. J Med Chem. 2007. PMID: 17880056
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
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
Plummer MS, Cornicelli J, Roark H, Skalitzky DJ, Stankovic CJ, Bove S, Pandit J, Goodman A, Hicks J, Shahripour A, Beidler D, Lu XK, Sanchez B, Whitehead C, Sarver R, Braden T, Gowan R, Shen XQ, Welch K, Ogden A, Sadagopan N, Baum H, Miller H, Banotai C, Spessard C, Lightle S. Plummer MS, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3438-42. doi: 10.1016/j.bmcl.2013.03.072. Epub 2013 Mar 28. Bioorg Med Chem Lett. 2013. PMID: 23582272
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy.
Plummer MS, Cornicelli J, Roark H, Skalitzky DJ, Stankovic CJ, Bove S, Pandit J, Goodman A, Hicks J, Shahripour A, Beidler D, Lu XK, Sanchez B, Whitehead C, Sarver R, Braden T, Gowan R, Shen XQ, Welch K, Ogden A, Sadagopan N, Baum H, Miller H, Banotai C, Spessard C, Lightle S. Plummer MS, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3443-7. doi: 10.1016/j.bmcl.2013.03.082. Epub 2013 Mar 29. Bioorg Med Chem Lett. 2013. PMID: 23597790
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: gowan rc. 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: gowan rc. Nat Med. 1999 Jul;5(7):810-6. doi: 10.1038/10533. Nat Med. 1999. PMID: 10395327
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Boys ML, Bian F, Kramer JB, Chio CL, Ren XD, Chen H, Barrett SD, Sexton KE, Iula DM, Filzen GF, Nguyen MN, Angell P, Downs VL, Wang Z, Raheja N, Ellsworth EL, Fakhoury S, Bratton LD, Keller PR, Gowan R, Drummond EM, Maiti SN, Hena MA, Lu L, McConnell P, Knafels JD, Thanabal V, Sun F, Alessi D, McCarthy A, Zhang E, Finzel BC, Patel S, Ciotti SM, Eisma R, Payne NA, Gilbertsen RB, Kostlan CR, Pocalyko DJ, Lala DS. Boys ML, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3392-7. doi: 10.1016/j.bmcl.2012.04.013. Epub 2012 Apr 10. Bioorg Med Chem Lett. 2012. PMID: 22542194