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Items: 15

1.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Stubbs MC, Burn TC, Sparks RB, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue C, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu P.

Clin Cancer Res. 2018 Sep 11. pii: clincanres.0098.2018. doi: 10.1158/1078-0432.CCR-18-0098. [Epub ahead of print]

PMID:
30206163
2.

Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications.

Diamond S, Boer J, Maduskuie TP Jr, Falahatpisheh N, Li Y, Yeleswaram S.

Drug Metab Dispos. 2010 Aug;38(8):1277-85. doi: 10.1124/dmd.110.032375. Epub 2010 Apr 26.

3.

Role of P-glycoprotein and the intestine in the excretion of DPC 333 [(2R)-2-{(3R)-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] in rodents.

Garner CE, Solon E, Lai CM, Lin J, Luo G, Jones K, Duan J, Decicco CP, Maduskuie T, Mercer SE, Gan LS, Qian M, Prakash S, Shen HS, Lee FW.

Drug Metab Dispos. 2008 Jun;36(6):1102-10. doi: 10.1124/dmd.107.017038. Epub 2008 Mar 17.

4.

Pharmacokinetics and pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a potent and selective inhibitor of tumor necrosis factor alpha-converting enzyme in rodents, dogs, chimpanzees, and humans.

Qian M, Bai SA, Brogdon B, Wu JT, Liu RQ, Covington MB, Vaddi K, Newton RC, Fossler MJ, Garner CE, Deng Y, Maduskuie T, Trzaskos J, Duan JJ, Decicco CP, Christ DD.

Drug Metab Dispos. 2007 Oct;35(10):1916-25. Epub 2007 Jul 26.

6.

Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.

Gilmore JL, King BW, Harris C, Maduskuie T, Mercer SE, Liu RQ, Covington MB, Qian M, Ribadeneria MD, Vaddi K, Trzaskos JM, Newton RC, Decicco CP, Duan JJ.

Bioorg Med Chem Lett. 2006 May 15;16(10):2699-704. Epub 2006 Mar 3.

PMID:
16516466
7.

Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.

Thompson LA, Liauw AY, Ramanjulu MM, Kasireddy-Polam P, Mercer SE, Maduskuie TP, Glicksman M, Roach AH, Meredith JE, Liu RQ, Combs AP, Higaki JN, Cordell B, Seiffert D, Zaczek RC, Robertson DW, Olson RE.

Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.

PMID:
16473009
8.

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.

Galemmo RA Jr, Wells BL, Rossi KA, Alexander RS, Dominguez C, Maduskuie TP, Stouten PF, Wright MR, Aungst BJ, Wong PC, Knabb RM, Wexler RR.

Bioorg Med Chem Lett. 2000 Feb 7;10(3):301-4.

PMID:
10698459
9.

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.

Galemmo RA Jr, Maduskuie TP, Dominguez C, Rossi KA, Knabb RM, Wexler RR, Stouten PF.

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2705-10.

PMID:
9873607
10.

Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.

Maduskuie TP Jr, McNamara KJ, Ru Y, Knabb RM, Stouten PF.

J Med Chem. 1998 Jan 1;41(1):53-62.

PMID:
9438022
11.

Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.

Maduskuie TP Jr, Wilde RG, Billheimer JT, Cromley DA, Germain S, Gillies PJ, Higley CA, Johnson AL, Pennev P, Shimshick EJ, et al.

J Med Chem. 1995 Mar 31;38(7):1067-83.

PMID:
7707310
12.

Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.

Higley CA, Wilde RG, Maduskuie TP, Johnson AL, Pennev P, Billheimer JT, Robinson CS, Gillies PJ, Wexler RR.

J Med Chem. 1994 Oct 14;37(21):3511-22.

PMID:
7932580
13.

Synthesis and in vitro LTD4 antagonist activity of bicyclic and monocyclic cyclopentylurethane and cyclopentylacetamide N-arylsulfonyl amides.

Matassa VG, Brown FJ, Bernstein PR, Shapiro HS, Maduskuie TP Jr, Cronk LA, Vacek EP, Yee YK, Snyder DW, Krell RD, et al.

J Med Chem. 1990 Sep;33(9):2621-9.

PMID:
2167983
14.

Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.

Matassa VG, Maduskuie TP Jr, Shapiro HS, Hesp B, Snyder DW, Aharony D, Krell RD, Keith RA.

J Med Chem. 1990 Jun;33(6):1781-90.

PMID:
2342072
15.

Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes.

Brown FJ, Bernstein PR, Cronk LA, Dosset DL, Hebbel KC, Maduskuie TP Jr, Shapiro HS, Vacek EP, Yee YK, Willard AK, et al.

J Med Chem. 1989 Apr;32(4):807-26.

PMID:
2704027

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