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Page 1
3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.
Djuric SW, BaMaung NY, Basha A, Liu H, Luly JR, Madar DJ, Sciotti RJ, Tu NP, Wagenaar FL, Wiedeman PE, Zhou X, Ballaron S, Bauch J, Chen YW, Chiou XG, Fey T, Gauvin D, Gubbins E, Hsieh GC, Marsh KC, Mollison KW, Pong M, Shaughnessy TK, Sheets MP, Smith M, Trevillyan JM, Warrior U, Wegner CD, Carter GW. Djuric SW, et al. Among authors: madar dj. J Med Chem. 2000 Aug 10;43(16):2975-81. doi: 10.1021/jm990615a. J Med Chem. 2000. PMID: 10956206
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: madar dj. J Med Chem. 2006 Jun 15;49(12):3520-35. doi: 10.1021/jm051283e. J Med Chem. 2006. PMID: 16759095
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM. Madar DJ, et al. J Med Chem. 2006 Oct 19;49(21):6416-20. doi: 10.1021/jm060777o. J Med Chem. 2006. PMID: 17034148
Inhibition of p56(lck) tyrosine kinase by isothiazolones.
Trevillyan JM, Chiou XG, Ballaron SJ, Tang QM, Buko A, Sheets MP, Smith ML, Putman CB, Wiedeman P, Tu N, Madar D, Smith HT, Gubbins EJ, Warrior UP, Chen YW, Mollison KW, Faltynek CR, Djurić SW. Trevillyan JM, et al. Arch Biochem Biophys. 1999 Apr 1;364(1):19-29. doi: 10.1006/abbi.1999.1099. Arch Biochem Biophys. 1999. PMID: 10087161
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: madar dj. J Med Chem. 2006 Nov 2;49(22):6439-42. doi: 10.1021/jm060955d. J Med Chem. 2006. PMID: 17064063
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM. Backes BJ, et al. Among authors: madar dj. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. doi: 10.1016/j.bmcl.2007.01.026. Epub 2007 Jan 19. Bioorg Med Chem Lett. 2007. PMID: 17276063
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.
Longenecker KL, Stewart KD, Madar DJ, Jakob CG, Fry EH, Wilk S, Lin CW, Ballaron SJ, Stashko MA, Lubben TH, Yong H, Pireh D, Pei Z, Basha F, Wiedeman PE, von Geldern TW, Trevillyan JM, Stoll VS. Longenecker KL, et al. Among authors: madar dj. Biochemistry. 2006 Jun 20;45(24):7474-82. doi: 10.1021/bi060184f. Biochemistry. 2006. PMID: 16768443
Prospects for pharmacologic inhibition of hepatic glucose production.
Kurukulasuriya R, Link JT, Madar DJ, Pei Z, Rohde JJ, Richards SJ, Souers AJ, Szczepankiewicz BG. Kurukulasuriya R, et al. Among authors: madar dj. Curr Med Chem. 2003 Jan;10(2):99-121. doi: 10.2174/0929867033368547. Curr Med Chem. 2003. PMID: 12570713 Review.
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.
Bruncko M, Tahir SK, Song X, Chen J, Ding H, Huth JR, Jin S, Judge RA, Madar DJ, Park CH, Park CM, Petros AM, Tse C, Rosenberg SH, Elmore SW. Bruncko M, et al. Among authors: madar dj. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7503-6. doi: 10.1016/j.bmcl.2010.10.010. Epub 2010 Oct 12. Bioorg Med Chem Lett. 2010. PMID: 21106457
15 results