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Items: 1 to 20 of 100

1.

Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.

Zhu GD, Gong J, Gandhi VB, Liu X, Shi Y, Johnson EF, Donawho CK, Ellis PA, Bouska JJ, Osterling DJ, Olson AM, Park C, Luo Y, Shoemaker A, Giranda VL, Penning TD.

Bioorg Med Chem. 2012 Aug 1;20(15):4635-45. doi: 10.1016/j.bmc.2012.06.021.

PMID:
22766219
2.
4.

Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

Tong Y, Bouska JJ, Ellis PA, Johnson EF, Leverson J, Liu X, Marcotte PA, Olson AM, Osterling DJ, Przytulinska M, Rodriguez LE, Shi Y, Soni N, Stavropoulos J, Thomas S, Donawho CK, Frost DJ, Luo Y, Giranda VL, Penning TD.

J Med Chem. 2009 Nov 12;52(21):6803-13. doi: 10.1021/jm900697r.

PMID:
19888760
5.

Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.

Zhu Q, Wang X, Chu Z, He G, Dong G, Xu Y.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):1993-6. doi: 10.1016/j.bmcl.2013.02.032.

PMID:
23481647
6.
7.

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.

J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j.

PMID:
19143569
8.

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.

Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL.

Bioorg Med Chem. 2008 Jul 15;16(14):6965-75. doi: 10.1016/j.bmc.2008.05.044.

PMID:
18541433
9.

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.

Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ, Webber SE, Curtin NJ.

Mol Cancer Ther. 2007 Mar;6(3):945-56.

10.

Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.

Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.

J Med Chem. 2010 Apr 22;53(8):3142-53. doi: 10.1021/jm901775y.

PMID:
20337371
11.

Discovery of 1-substituted benzyl-quinazoline-2,4(1H,3H)-dione derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors.

Yao H, Ji M, Zhu Z, Zhou J, Cao R, Chen X, Xu B.

Bioorg Med Chem. 2015 Feb 15;23(4):681-93. doi: 10.1016/j.bmc.2014.12.071.

PMID:
25614115
12.

Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor.

Liu X, Shi Y, Maag DX, Palma JP, Patterson MJ, Ellis PA, Surber BW, Ready DB, Soni NB, Ladror US, Xu AJ, Iyer R, Harlan JE, Solomon LR, Donawho CK, Penning TD, Johnson EF, Shoemaker AR.

Clin Cancer Res. 2012 Jan 15;18(2):510-23. doi: 10.1158/1078-0432.CCR-11-1973.

13.

Multi-targeted organometallic ruthenium(II)-arene anticancer complexes bearing inhibitors of poly(ADP-ribose) polymerase-1: A strategy to improve cytotoxicity.

Wang Z, Qian H, Yiu SM, Sun J, Zhu G.

J Inorg Biochem. 2014 Feb;131:47-55. doi: 10.1016/j.jinorgbio.2013.10.017.

PMID:
24239912
14.

Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.

Canan Koch SS, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li J, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z.

J Med Chem. 2002 Nov 7;45(23):4961-74.

PMID:
12408707
15.

Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.

White AW, Almassy R, Calvert AH, Curtin NJ, Griffin RJ, Hostomsky Z, Maegley K, Newell DR, Srinivasan S, Golding BT.

J Med Chem. 2000 Nov 2;43(22):4084-97.

PMID:
11063605
16.

New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.

Zhu HY, Desai J, Cooper AB, Wang J, Rane DF, Kirschmeier P, Strickland C, Liu M, Nomeir AA, Girijavallabhan VM.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1228-31. doi: 10.1016/j.bmcl.2013.12.046.

PMID:
24462667
17.

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.

Clin Cancer Res. 2007 May 1;13(9):2728-37.

18.

Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.

Giannini G, Battistuzzi G, Vesci L, Milazzo FM, De Paolis F, Barbarino M, Guglielmi MB, Carollo V, Gallo G, Artali R, Dallavalle S.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):462-6. doi: 10.1016/j.bmcl.2013.12.048.

PMID:
24388690
19.

Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.

Scarpelli R, Boueres JK, Cerretani M, Ferrigno F, Ontoria JM, Rowley M, Schultz-Fademrecht C, Toniatti C, Jones P.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):488-92. doi: 10.1016/j.bmcl.2009.11.127.

PMID:
20007017
20.

Platinated benzonaphthyridone is a stronger inhibitor of poly(ADP-ribose) polymerase-1 and a more potent anticancer agent than is the parent inhibitor.

Wang B, Qian H, Yiu SM, Sun J, Zhu G.

Eur J Med Chem. 2014 Jan;71:366-73. doi: 10.1016/j.ejmech.2013.10.062.

PMID:
24361480

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