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Items: 1 to 20 of 113

1.

SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.

Karra S, Xiao Y, Chen X, Liu-Bujalski L, Huck B, Sutton A, Goutopoulos A, Askew B, Josephson K, Jiang X, Shutes A, Shankar V, Noonan T, Garcia-Berrios G, Dong R, Dhanabal M, Tian H, Wang Z, Clark A, Goodstal S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3081-7. doi: 10.1016/j.bmcl.2013.03.008. Epub 2013 Mar 13.

PMID:
23570792
2.

AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues.

Juan G, Bush TL, Ma C, Manoukian R, Chung G, Hawkins JM, Zoog S, Kendall R, Radinsky R, Loberg R, Friberg G, Payton M.

J Transl Med. 2014 Nov 4;12:307. doi: 10.1186/s12967-014-0307-x.

3.

Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.

Payton M, Bush TL, Chung G, Ziegler B, Eden P, McElroy P, Ross S, Cee VJ, Deak HL, Hodous BL, Nguyen HN, Olivieri PR, Romero K, Schenkel LB, Bak A, Stanton M, Dussault I, Patel VF, Geuns-Meyer S, Radinsky R, Kendall RL.

Cancer Res. 2010 Dec 1;70(23):9846-54. doi: 10.1158/0008-5472.CAN-10-3001. Epub 2010 Oct 8.

4.

Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.

Kim KH, Wissner A, Floyd MB Jr, Fraser HL, Wang YD, Dushin RG, Hu Y, Olland A, Guo B, Arndt K.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5225-8. doi: 10.1016/j.bmcl.2009.07.007. Epub 2009 Jul 8.

PMID:
19628388
5.

A thienopyrimidine derivative induces growth inhibition and apoptosis in human cancer cell lines via inhibiting Aurora B kinase activity.

Li J, Hu H, Lang Q, Zhang H, Huang Q, Wu Y, Yu L.

Eur J Med Chem. 2013 Jul;65:151-7. doi: 10.1016/j.ejmech.2013.04.058. Epub 2013 May 4.

PMID:
23707920
6.

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.

Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14.

PMID:
21802948
7.

Investigation on the 1,6-naphthyridine motif: discovery and SAR study of 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one-based c-Met kinase inhibitors.

Wang Y, Xu ZL, Ai J, Peng X, Lin JP, Ji YC, Geng MY, Long YQ.

Org Biomol Chem. 2013 Mar 7;11(9):1545-62. doi: 10.1039/c2ob26710a.

PMID:
23188156
8.

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.

9.

Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor.

Farrell P, Shi L, Matuszkiewicz J, Balakrishna D, Hoshino T, Zhang L, Elliott S, Fabrey R, Lee B, Halkowycz P, Sang B, Ishino S, Nomura T, Teratani M, Ohta Y, Grimshaw C, Paraselli B, Satou T, de Jong R.

Mol Cancer Ther. 2013 Apr;12(4):460-70. doi: 10.1158/1535-7163.MCT-12-0657. Epub 2013 Jan 28.

10.

Jadomycin B, an Aurora-B kinase inhibitor discovered through virtual screening.

Fu DH, Jiang W, Zheng JT, Zhao GY, Li Y, Yi H, Li ZR, Jiang JD, Yang KQ, Wang Y, Si SY.

Mol Cancer Ther. 2008 Aug;7(8):2386-93. doi: 10.1158/1535-7163.MCT-08-0035.

11.

TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens.

Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E.

Mol Cancer Ther. 2012 Mar;11(3):700-9. doi: 10.1158/1535-7163.MCT-11-0762. Epub 2011 Dec 21.

12.

Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as aurora kinase inhibitors.

Defaux J, Antoine M, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P.

ChemMedChem. 2014 Jan;9(1):217-32. doi: 10.1002/cmdc.201300384. Epub 2013 Nov 24.

PMID:
24273104
13.

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.

Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. Epub 2005 Dec 5.

PMID:
16337122
14.

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL, Heathcote M, Maman S, Matthews JE, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Rees DC, Reule M, Tisi D, Williams G, Vinković M, Wyatt PG.

J Med Chem. 2009 Jan 22;52(2):379-88. doi: 10.1021/jm800984v.

PMID:
19143567
15.

Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.

Defaux J, Antoine M, Logé C, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52. doi: 10.1016/j.bmcl.2014.06.078. Epub 2014 Jul 3.

PMID:
25022204
16.

SAR156497, an exquisitely selective inhibitor of aurora kinases.

Carry JC, Clerc F, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abécassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Rommé B, Murer M, Gontier S, Prévost C, Monteiro ML, Combeau C.

J Med Chem. 2015 Jan 8;58(1):362-75. doi: 10.1021/jm501326k. Epub 2014 Nov 24.

PMID:
25369539
17.

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21.

PMID:
20833547
18.

A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.

Rawson TE, Rüth M, Blackwood E, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Georges GJ, Goller B, Halladay J, Hunsaker T, Kleinheinz T, Krell HW, Li J, Liang J, Limberg A, McNutt A, Moffat J, Phillips G, Ran Y, Safina B, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhou A, Zhu BY, Rüger P, Cochran AG.

J Med Chem. 2008 Aug 14;51(15):4465-75. doi: 10.1021/jm800052b. Epub 2008 Jul 17.

PMID:
18630890
19.

Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.

Cee VJ, Schenkel LB, Hodous BL, Deak HL, Nguyen HN, Olivieri PR, Romero K, Bak A, Be X, Bellon S, Bush TL, Cheng AC, Chung G, Coats S, Eden PM, Hanestad K, Gallant PL, Gu Y, Huang X, Kendall RL, Lin MH, Morrison MJ, Patel VF, Radinsky R, Rose PE, Ross S, Sun JR, Tang J, Zhao H, Payton M, Geuns-Meyer SD.

J Med Chem. 2010 Sep 9;53(17):6368-77. doi: 10.1021/jm100394y.

PMID:
20684549
20.

Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.

Voss ME, Rainka MP, Fleming M, Peterson LH, Belanger DB, Siddiqui MA, Hruza A, Voigt J, Gray K, Basso AD.

Bioorg Med Chem Lett. 2012 May 15;22(10):3544-9. doi: 10.1016/j.bmcl.2012.03.051. Epub 2012 Mar 21.

PMID:
22503250

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