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Items: 15

1.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR.

Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1.

2.

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14.

3.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25.

PMID:
25582600
4.

Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione γ-secretase modulators.

Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Xie L, Zhang L, Pustilnik LR, Vetelino BC, Wood KM, Pozdnyakov N, Verhoest PR, O'Donnell CJ.

J Med Chem. 2014 Feb 13;57(3):1046-62. doi: 10.1021/jm401782h. Epub 2014 Jan 28.

PMID:
24428186
5.

Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators.

Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Lira R, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Vetelino BC, Xie L, Zhang L, Pustilnik LR, Wood KM, O'Donnell CJ.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2906-11. doi: 10.1016/j.bmcl.2012.02.059. Epub 2012 Mar 1.

PMID:
22429469
6.

Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.

Stepan AF, Subramanyam C, Efremov IV, Dutra JK, O'Sullivan TJ, DiRico KJ, McDonald WS, Won A, Dorff PH, Nolan CE, Becker SL, Pustilnik LR, Riddell DR, Kauffman GW, Kormos BL, Zhang L, Lu Y, Capetta SH, Green ME, Karki K, Sibley E, Atchison KP, Hallgren AJ, Oborski CE, Robshaw AE, Sneed B, O'Donnell CJ.

J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29.

PMID:
22420884
7.

Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.

Stepan AF, Karki K, McDonald WS, Dorff PH, Dutra JK, Dirico KJ, Won A, Subramanyam C, Efremov IV, O'Donnell CJ, Nolan CE, Becker SL, Pustilnik LR, Sneed B, Sun H, Lu Y, Robshaw AE, Riddell D, O'Sullivan TJ, Sibley E, Capetta S, Atchison K, Hallgren AJ, Miller E, Wood A, Obach RS.

J Med Chem. 2011 Nov 24;54(22):7772-83. doi: 10.1021/jm200893p. Epub 2011 Oct 26.

PMID:
21995460
8.

Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.

Lu Y, Zhang L, Nolan CE, Becker SL, Atchison K, Robshaw AE, Pustilnik LR, Osgood SM, Miller EH, Stepan AF, Subramanyam C, Efremov I, Hallgren AJ, Riddell D.

J Pharmacol Exp Ther. 2011 Dec;339(3):922-34. doi: 10.1124/jpet.111.186791. Epub 2011 Sep 19.

PMID:
21930801
9.

Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor.

Jani JP, Finn RS, Campbell M, Coleman KG, Connell RD, Currier N, Emerson EO, Floyd E, Harriman S, Kath JC, Morris J, Moyer JD, Pustilnik LR, Rafidi K, Ralston S, Rossi AM, Steyn SJ, Wagner L, Winter SM, Bhattacharya SK.

Cancer Res. 2007 Oct 15;67(20):9887-93.

10.

An inhibitor of the epidermal growth factor receptor function does not affect the ability of human papillomavirus 11 to form warts in the xenografted immunodeficient mouse model.

Parkinson T, Howett MK, Welsh PA, Patrick SD, Neely EB, Flanagan N, Pollack VA, Pustilnik LR, Moyer J, Perros M.

Antiviral Res. 2007 Apr;74(1):43-50. Epub 2007 Jan 9.

PMID:
17239450
11.

The biological and biochemical effects of CP-654577, a selective erbB2 kinase inhibitor, on human breast cancer cells.

Barbacci EG, Pustilnik LR, Rossi AM, Emerson E, Miller PE, Boscoe BP, Cox ED, Iwata KK, Jani JP, Provoncha K, Kath JC, Liu Z, Moyer JD.

Cancer Res. 2003 Aug 1;63(15):4450-9.

12.

Achieving selectivity between highly homologous tyrosine kinases: a novel selective erbB2 inhibitor.

Bhattacharya SK, Cox ED, Kath JC, Mathiowetz AM, Morris J, Moyer JD, Pustilnik LR, Rafidi K, Richter DT, Su C, Wessel MD.

Biochem Biophys Res Commun. 2003 Jul 25;307(2):267-73.

PMID:
12859950
13.

Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography.

Wright SW, Carlo AA, Carty MD, Danley DE, Hageman DL, Karam GA, Levy CB, Mansour MN, Mathiowetz AM, McClure LD, Nestor NB, McPherson RK, Pandit J, Pustilnik LR, Schulte GK, Soeller WC, Treadway JL, Wang IK, Bauer PH.

J Med Chem. 2002 Aug 29;45(18):3865-77.

PMID:
12190310
14.

Inhibition of epidermal growth factor receptor-associated tyrosine phosphorylation in human carcinomas with CP-358,774: dynamics of receptor inhibition in situ and antitumor effects in athymic mice.

Pollack VA, Savage DM, Baker DA, Tsaparikos KE, Sloan DE, Moyer JD, Barbacci EG, Pustilnik LR, Smolarek TA, Davis JA, Vaidya MP, Arnold LD, Doty JL, Iwata KK, Morin MJ.

J Pharmacol Exp Ther. 1999 Nov;291(2):739-48.

PMID:
10525095
15.

Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase.

Moyer JD, Barbacci EG, Iwata KK, Arnold L, Boman B, Cunningham A, DiOrio C, Doty J, Morin MJ, Moyer MP, Neveu M, Pollack VA, Pustilnik LR, Reynolds MM, Sloan D, Theleman A, Miller P.

Cancer Res. 1997 Nov 1;57(21):4838-48.

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