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Items: 31

1.

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020. Epub 2018 Apr 11.

PMID:
29678460
2.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.

J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12.

PMID:
28949521
3.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF.

J Med Chem. 2017 May 11;60(9):3828-3850. doi: 10.1021/acs.jmedchem.7b00017. Epub 2017 Apr 21.

PMID:
28368119
4.

Methylpyrrole inhibitors of BET bromodomains.

Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF.

Bioorg Med Chem Lett. 2017 May 15;27(10):2225-2233. doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24.

PMID:
28268136
5.

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.

Leverson JD, Phillips DC, Mitten MJ, Boghaert ER, Diaz D, Tahir SK, Belmont LD, Nimmer P, Xiao Y, Ma XM, Lowes KN, Kovar P, Chen J, Jin S, Smith M, Xue J, Zhang H, Oleksijew A, Magoc TJ, Vaidya KS, Albert DH, Tarrant JM, La N, Wang L, Tao ZF, Wendt MD, Sampath D, Rosenberg SH, Tse C, Huang DC, Fairbrother WJ, Elmore SW, Souers AJ.

Sci Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642.

PMID:
25787766
6.

Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH, Chen Z, Frey RR, Johnson EF, Osterling DJ, Olson AM, Bouska JJ, Luo Y, Curtin ML, Donawho CK, Michaelides MR, Tse C, Davidsen SK, Albert DH.

J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. doi: 10.1124/jpet.112.197087. Epub 2012 Aug 30.

PMID:
22935731
7.

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Ji Z, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Soni NB, Magoc TJ, Stewart KD, Wei RQ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4528-31. doi: 10.1016/j.bmcl.2012.05.125. Epub 2012 Jun 7.

PMID:
22727637
8.

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26.

PMID:
22695126
9.

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12. doi: 10.1016/j.bmcl.2012.03.035. Epub 2012 Mar 14.

PMID:
22465635
10.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

McClellan WJ, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Magoc TJ, Marcotte PA, Osterling DJ, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5620-4. doi: 10.1016/j.bmcl.2011.06.041. Epub 2011 Jun 29.

PMID:
21778056
11.

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.

Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK.

Mol Cancer Ther. 2006 Apr;5(4):995-1006.

12.

Alpha-keto amides as inhibitors of histone deacetylase.

Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.

PMID:
12951120
13.

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Curtin ML, Florjancic AS, Heyman HR, Michaelides MR, Garland RB, Holms JH, Steinman DH, Dellaria JF, Gong J, Wada CK, Guo Y, Elmore IB, Tapang P, Albert DH, Magoc TJ, Marcotte PA, Bouska JJ, Goodfellow CL, Bauch JL, Marsh KC, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60.

PMID:
11412980
14.

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

Michaelides MR, Dellaria JF, Gong J, Holms JH, Bouska JJ, Stacey J, Wada CK, Heyman HR, Curtin ML, Guo Y, Goodfellow CL, Elmore IB, Albert DH, Magoc TJ, Marcotte PA, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1553-6.

PMID:
11412979
15.

Evaluation of the inhibition of other metalloproteinases by matrix metalloproteinase inhibitors.

Marcotte PA, Elmore IN, Guan Z, Magoc TJ, Albert DH, Morgand DW, Curtin ML, Garland RB, Guo Y, Heyman HR, Holms JH, Sheppard GS, Steinman DH, Wada CK, Davidsen SK.

J Enzyme Inhib. 1999;14(6):425-35.

PMID:
10536876
16.

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

Sheppard GS, Florjancic AS, Giesler JR, Xu L, Guo Y, Davidsen SK, Marcotte PA, Elmore I, Albert DH, Magoc TJ, Bouska JJ, Goodfellow CL, Morgan DW, Summers JB.

Bioorg Med Chem Lett. 1998 Nov 17;8(22):3251-6.

PMID:
9873712
17.

The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.

Steinman DH, Curtin ML, Garland RB, Davidsen SK, Heyman HR, Holms JH, Albert DH, Magoc TJ, Nagy IB, Marcotte PA, Li J, Morgan DW, Hutchins C, Summers JB.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2087-92.

PMID:
9873491
18.

Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.

Curtin ML, Garland RB, Davidsen SK, Marcotte PA, Albert DH, Magoc TJ, Hutchins C.

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8.

PMID:
9873367
19.

Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.

Curtin ML, Davidsen SK, Heyman HR, Garland RB, Sheppard GS, Florjancic AS, Xu L, Carrera GM Jr, Steinman DH, Trautmann JA, Albert DH, Magoc TJ, Tapang P, Rhein DA, Conway RG, Luo G, Denissen JF, Marsh KC, Morgan DW, Summers JB.

J Med Chem. 1998 Jan 1;41(1):74-95.

PMID:
9438024
20.

Ex vivo inhibition of beta-thromboglobulin release following administration to man of ABT-299, a novel prodrug of a potent platelet activating factor antagonist.

Albert DH, Magoc TJ, Menacherry SD, Morgan DW, Sun E, Reyes AE, Kleinert HD, Carter GW, Summers JB.

Inflamm Res. 1997 Jul;46(7):272-7.

PMID:
9266276
21.

Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist.

Albert DH, Magoc TJ, Tapang P, Luo G, Morgan DW, Curtin M, Sheppard GS, Xu L, Heyman HR, Davidsen SK, Summers JB, Carter GW.

Eur J Pharmacol. 1997 Apr 23;325(1):69-80.

PMID:
9151941
22.

ABT-299, a novel PAF antagonist, attenuates multiple effects of endotoxemia in conscious rats.

Albert DH, Luo G, Magoc TJ, Tapang P, Holms JH, Davidsen SK, Summers JB, Carter GW.

Shock. 1996 Aug;6(2):112-7.

PMID:
8856845
23.

Properties of ABT-299, a prodrug of A-85783, a highly potent platelet activating factor receptor antagonist.

Albert DH, Conway RG, Magoc TJ, Tapang P, Rhein DA, Luo G, Holms JH, Davidsen SK, Summers JB, Carter GW.

J Pharmacol Exp Ther. 1996 Jun;277(3):1595-606.

PMID:
8667228
24.

Ex vivo inhibition of PAF-induced beta-thromboglobulin release in man by ABT-299, a potent PAF antagonist.

Albert DH, Magoc TJ, Kleinert HD, Sun E, Reyes AE, Carter GW, Summers JB.

Adv Exp Med Biol. 1996;416:381-7. No abstract available.

PMID:
9131177
25.

ABT-299, a potent antagonist of platelet activating factor.

Summers JB, Albert DH, Davidsen SK, Conway RG, Holms JH, Magoc TJ, Luo G, Tapang P, Rhein DA, Carter GW.

Adv Prostaglandin Thromboxane Leukot Res. 1995;23:475-7. No abstract available.

PMID:
7732895
26.

N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.

Davidsen SK, Summers JB, Albert DH, Holms JH, Heyman HR, Magoc TJ, Conway RG, Rhein DA, Carter GW.

J Med Chem. 1994 Dec 23;37(26):4423-9.

PMID:
7799395
27.

Spontaneous bronchopneumonia in laboratory dogs infected with untyped Mycoplasma spp.

Kirchner BK, Port CD, Magoc TJ, Sidor MA, Ruben Z.

Lab Anim Sci. 1990 Nov;40(6):625-8.

PMID:
2172628
28.

Pasteurella pneumotropica in rabbits from a "Pasteurella-free" production colony.

Kirchner BK, Magoc TJ, Sidor MA.

Lab Anim Sci. 1983 Oct;33(5):461-2.

PMID:
6227773
29.

Development of a new in vivo anaphylactic histamine release assay in rats.

Butchko GM, Magoc TJ, Aspinall RL, Nakao A.

Immunol Lett. 1982 Jan;4(1):45-8.

PMID:
6174429
30.

The influence upon mitogenic and cellular immunologic reactive systems in vitro by poly(I:C) and BCG murine interferons induced in vivo.

Clinton BA, Magoc TJ, Aspinall RL, Rapoza NP.

Cell Immunol. 1976 Nov;27(1):60-70. No abstract available.

PMID:
136302
31.

The abrogation of macrophage migration inhibition by pretreatment of immune exudate cells with anti-theta antibody and complement.

Clinton BA, Magoc TJ, Aspinall RL.

J Immunol. 1974 May;112(5):1741-6. No abstract available.

PMID:
4594414

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