Publications by authors named "Mark Albom"

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Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
Gregory R Ott, Mangeng Cheng, Keith S Learn, Jason Wagner, Diane E Gingrich, Mark S Albom

J Med Chem· August 2016

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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.
Eugen F Mesaros, Thelma S Angeles, Mark S Albom, Jason C Wagner, Lisa D Aimone

Bioorg Med Chem Lett· March 2015

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Time-resolved fluorescence resonance energy transfer as a versatile tool in the development of homogeneous cellular kinase assays.
Lisa Saville, Chrysanthe Spais, Jennifer L Mason, Mark S Albom, Seetha Murthy

Assay Drug Dev Technol· December 2012

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Comparison of LanthaScreen Eu kinase binding assay and surface plasmon resonance method in elucidating the binding kinetics of focal adhesion kinase inhibitors.
Jennifer L Mason, Chrysanthe Spais, Jean Husten, Eric Prouty, Mark S Albom

Assay Drug Dev Technol· October 2012

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A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.
Benjamin J Dugan, Diane E Gingrich, Eugen F Mesaros, Karen L Milkiewicz, Matthew A Curry, Mark S Albom

J Med Chem· June 2012

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Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Diane E Gingrich, Joseph G Lisko, Matthew A Curry, Mangeng Cheng, Matthew Quail, Mark S Albom

J Med Chem· May 2012

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CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
Mangeng Cheng, Matthew R Quail, Diane E Gingrich, Gregory R Ott, Lihui Lu, Mark S Albom

Mol Cancer Ther· March 2012

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Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Eugen F Mesaros, Tho V Thieu, Gregory J Wells, Craig A Zificsak, Jason C Wagner, Mark S Albom

J Med Chem· January 2012

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Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Robert L Hudkins, Nadine C Becknell, Allison L Zulli, Ted L Underiner, Thelma S Angeles, Mark S Albom

J Med Chem· January 2012

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Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.
Craig A Zificsak, Diane E Gingrich, Henry J Breslin, Derek D Dunn, Karen L Milkiewicz, Mark S Albom

Bioorg Med Chem Lett· January 2012

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Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,⁷.1⁹,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.
Henry J Breslin, Brandon M Lane, Gregory R Ott, Arup K Ghose, Thelma S Angeles, Mark S Albom

J Med Chem· January 2012

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2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Linda R Weinberg, Mark S Albom, Thelma S Angeles, Henry J Breslin, Diane E Gingrich

Bioorg Med Chem Lett· December 2011

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Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.
Rabindranath Tripathy, Robert J McHugh, Arup K Ghose, Gregory R Ott, Thelma S Angeles, Mark S Albom

Bioorg Med Chem Lett· December 2011

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Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.
Karen L Milkiewicz, Lisa D Aimone, Mark S Albom, Thelma S Angeles, Hong Chang

Bioorg Med Chem· November 2011

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Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2.
Lily D Lu, Kristine L Stump, Nate H Wallace, Pawel Dobrzanski, Cynthia Serdikoff, Mark S Albom

J Immunol· October 2011

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2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Gregory R Ott, Gregory J Wells, Tho V Thieu, Matthew R Quail, Joseph G Lisko, Mark S Albom

J Med Chem· September 2011

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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.
Craig A Zificsak, Jay P Theroff, Lisa D Aimone, Thelma S Angeles, Mark S Albom

Bioorg Med Chem Lett· July 2011

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A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis.
Kristine L Stump, Lily D Lu, Pawel Dobrzanski, Cynthia Serdikoff, Diane E Gingrich, Mark S Albom

Arthritis Res Ther· April 2011

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Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Eugen F Mesaros, Jason P Burke, Jonathan D Parrish, Benjamin J Dugan, Andrew V Anzalone, Mark S Albom

Bioorg Med Chem Lett· January 2011

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Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.
Linda R Weinberg, Mark S Albom, Thelma S Angeles, Jean Husten, Joseph G Lisko

Bioorg Med Chem Lett· January 2011

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2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.
Craig A Zificsak, Jay P Theroff, Lisa D Aimone, Mark S Albom, Thelma S Angeles

Bioorg Med Chem Lett· January 2011

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Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
Gregory R Ott, Rabindranath Tripathy, Mangeng Cheng, Robert McHugh, Andrew V Anzalone, Mark S Albom

ACS Med Chem Lett· December 2010

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Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Karen L Milkiewicz, Linda R Weinberg, Mark S Albom, Thelma S Angeles, Mangeng Cheng

Bioorg Med Chem· June 2010

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ALK mutants in the kinase domain exhibit altered kinase activity and differential sensitivity to small molecule ALK inhibitors.
Lihui Lu, Arup K Ghose, Matthew R Quail, Mark S Albom, John T Durkin

Biochemistry· April 2009

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TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.
Ted L Underiner, Bruce Ruggeri, Lisa Aimone, Mark Albom, Thelma Angeles

Bioorg Med Chem Lett· April 2008

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