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Page 1
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Penning TD, et al. J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j. J Med Chem. 2009. PMID: 19143569
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
Penning TD, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, Graneto MJ, Lee LF, Malecha JW, Miyashiro JM, Rogers RS, Rogier DJ, Yu SS, AndersonGD, Burton EG, Cogburn JN, Gregory SA, Koboldt CM, Perkins WE, Seibert K, Veenhuizen AW, Zhang YY, Isakson PC. Penning TD, et al. J Med Chem. 1997 Apr 25;40(9):1347-65. doi: 10.1021/jm960803q. J Med Chem. 1997. PMID: 9135032
Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.
Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG. Penning TD, et al. J Med Chem. 2000 Feb 24;43(4):721-35. doi: 10.1021/jm990496z. J Med Chem. 2000. PMID: 10691697
Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.
Penning TD, Russell MA, Chen BB, Chen HY, Liang CD, Mahoney MW, Malecha JW, Miyashiro JM, Yu SS, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG. Penning TD, et al. J Med Chem. 2002 Aug 1;45(16):3482-90. doi: 10.1021/jm0200916. J Med Chem. 2002. PMID: 12139459
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG. Penning TD, et al. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3383-6. doi: 10.1016/s0960-894x(02)00760-6. Bioorg Med Chem Lett. 2002. PMID: 12419366
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG. Penning TD, et al. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1137-9. doi: 10.1016/s0960-894x(03)00039-8. Bioorg Med Chem Lett. 2003. PMID: 12643929
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.
Penning TD, Khilevich A, Chen BB, Russell MA, Boys ML, Wang Y, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Rader RK, Settle SL, Shannon KE, Steininger CN, Westlin MM, Westlin WF. Penning TD, et al. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3156-61. doi: 10.1016/j.bmcl.2006.03.045. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621534
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models.
Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE, Ferguson DC, Ghoreishi-Haack NS, Grimm DR, Guan R, Han EK, Holley-Shanks RR, Hristov B, Idler KB, Jarvis K, Johnson EF, Kleinberg LR, Klinghofer V, Lasko LM, Liu X, Marsh KC, McGonigal TP, Meulbroek JA, Olson AM, Palma JP, Rodriguez LE, Shi Y, Stavropoulos JA, Tsurutani AC, Zhu GD, Rosenberg SH, Giranda VL, Frost DJ. Donawho CK, et al. Among authors: penning td. Clin Cancer Res. 2007 May 1;13(9):2728-37. doi: 10.1158/1078-0432.CCR-06-3039. Clin Cancer Res. 2007. PMID: 17473206
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.
Zhu GD, Gandhi VB, Gong J, Thomas S, Woods KW, Song X, Li T, Diebold RB, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Bouska J, Olson A, Marsh KC, Stoll VS, Mamo M, Polakowski J, Campbell TJ, Martin RL, Gintant GA, Penning TD, Li Q, Rosenberg SH, Giranda VL. Zhu GD, et al. Among authors: penning td. J Med Chem. 2007 Jun 28;50(13):2990-3003. doi: 10.1021/jm0701019. Epub 2007 May 25. J Med Chem. 2007. PMID: 17523610
49 results