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Items: 16

1.

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.

Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L.

J Med Chem. 2019 Aug 15. doi: 10.1021/acs.jmedchem.9b00794. [Epub ahead of print]

PMID:
31368705
2.

Targeting kinases with precision.

Gardino AK, Evans EK, Kim JL, Brooijmans N, Hodous BL, Wolf B, Lengauer C.

Mol Cell Oncol. 2018 Apr 11;5(3):e1435183. doi: 10.1080/23723556.2018.1435183. eCollection 2018.

3.

A precision therapy against cancers driven by KIT/PDGFRA mutations.

Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K, DiPietro L, Zhang Y, Brooijmans N, LaBranche TP, Wozniak A, Gebreyohannes YK, Schöffski P, Heinrich MC, DeAngelo DJ, Miller S, Wolf B, Kohl N, Guzi T, Lydon N, Boral A, Lengauer C.

Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. doi: 10.1126/scitranslmed.aao1690.

PMID:
29093181
4.

Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines.

Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M.

J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31.

PMID:
25970324
5.

Synthesis of 4-substituted chlorophthalazines, dihydrobenzoazepinediones, 2-pyrazolylbenzoic acid, and 2-pyrazolylbenzohydrazide via 3-substituted 3-hydroxyisoindolin-1-ones.

Nguyen HN, Cee VJ, Deak HL, Du B, Faber KP, Gunaydin H, Hodous BL, Hollis SL, Krolikowski PH, Olivieri PR, Patel VF, Romero K, Schenkel LB, Geuns-Meyer SD.

J Org Chem. 2012 Apr 20;77(8):3887-906. doi: 10.1021/jo3000628. Epub 2012 Apr 5.

PMID:
22458369
6.

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.

7.

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
8.

Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.

Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20.

PMID:
19062275
9.

N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.

Deak HL, Newcomb JR, Nunes JJ, Boucher C, Cheng AC, DiMauro EF, Epstein LF, Gallant P, Hodous BL, Huang X, Lee JH, Patel VF, Schneider S, Turci SM, Zhu X.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1172-6. Epub 2007 Dec 5.

PMID:
18083554
10.

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.

Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H.

Bioorg Med Chem Lett. 2007 May 15;17(10):2886-9. Epub 2007 Feb 25.

PMID:
17350837
11.

Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.

Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H.

J Med Chem. 2007 Feb 22;50(4):627-40. Epub 2007 Jan 25.

PMID:
17253679
12.

Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.

Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Bready J, Caenepeel S, Cee VJ, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Tempest P, Wang L, Whittington DA, Zhao H.

J Med Chem. 2007 Feb 22;50(4):611-26. Epub 2007 Jan 25.

PMID:
17253678
13.

Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.

DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, White RD, Zhao H, Zhu L, Zhu X.

J Med Chem. 2006 Sep 21;49(19):5671-86.

PMID:
16970394
14.
16.

Enantioselective Staudinger synthesis of beta-lactams catalyzed by a planar-chiral nucleophile.

Hodous BL, Fu GC.

J Am Chem Soc. 2002 Feb 27;124(8):1578-9.

PMID:
11853423

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