Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK)
Ott, Gregory R, Cheng, Mangeng, Learn, Keith S, Wagner, Jason, Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew, Mesaros, Eugen F, Ghose, Arup K, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Dobrzanski, Pawel, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin, Huang, Zeqi, Aimone, Lisa D, Bruckheimer, Elizabeth, Anderson, Nathan, Friedman, Jay, Fernandez, Sandra V, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D
Published in Journal of medicinal chemistry (25.08.2016)
Published in Journal of medicinal chemistry (25.08.2016)
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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
Stump, Kristine L, Lu, Lily D, Dobrzanski, Pawel, Serdikoff, Cynthia, Gingrich, Diane E, Dugan, Ben J, Angeles, Thelma S, Albom, Mark S, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce A, Seavey, Matthew M
Published in Arthritis research & therapy (21.04.2011)
Published in Arthritis research & therapy (21.04.2011)
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Journal Article
Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2
Lu, Lily D, Stump, Kristine L, Wallace, Nate H, Dobrzanski, Pawel, Serdikoff, Cynthia, Gingrich, Diane E, Dugan, Benjamin J, Angeles, Thelma S, Albom, Mark S, Mason, Jennifer L, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce A, Seavey, Matthew M
Published in The Journal of immunology (1950) (01.10.2011)
Published in The Journal of immunology (1950) (01.10.2011)
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Journal Article
CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers
Cheng, Mangeng, Quail, Matthew R, Gingrich, Diane E, Ott, Gregory R, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Cristofani, Flavio, Machiorlatti, Rodolfo, Abele, Cristina, Ator, Mark A, Dorsey, Bruce D, Inghirami, Giorgio, Ruggeri, Bruce A
Published in Molecular cancer therapeutics (01.03.2012)
Published in Molecular cancer therapeutics (01.03.2012)
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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
Dugan, Benjamin J, Gingrich, Diane E, Mesaros, Eugen F, Milkiewicz, Karen L, Curry, Matthew A, Zulli, Allison L, Dobrzanski, Pawel, Serdikoff, Cynthia, Jan, Mahfuza, Angeles, Thelma S, Albom, Mark S, Mason, Jennifer L, Aimone, Lisa D, Meyer, Sheryl L, Huang, Zeqi, Wells-Knecht, Kevin J, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D
Published in Journal of medicinal chemistry (14.06.2012)
Published in Journal of medicinal chemistry (14.06.2012)
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Journal Article
Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase
Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew A, Cheng, Mangeng, Quail, Matthew, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Haltiwanger, R. Curtis, Wells-Knecht, Kevin, Ott, Gregory R, Ghose, Arup K, Ator, Mark A, Ruggeri, Bruce, Dorsey, Bruce D
Published in Journal of medicinal chemistry (24.05.2012)
Published in Journal of medicinal chemistry (24.05.2012)
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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
Hudkins, Robert L, Becknell, Nadine C, Zulli, Allison L, Underiner, Ted L, Angeles, Thelma S, Aimone, Lisa D, Albom, Mark S, Chang, Hong, Miknyoczki, Sheila J, Hunter, Kathryn, Jones-Bolin, Susan, Zhao, Hugh, Bacon, Edward R, Mallamo, John P, Ator, Mark A, Ruggeri, Bruce A
Published in Journal of medicinal chemistry (26.01.2012)
Published in Journal of medicinal chemistry (26.01.2012)
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Journal Article
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
Breslin, Henry J, Lane, Brandon M, Ott, Gregory R, Ghose, Arup K, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Wan, Weihua, Haltiwanger, R. Curtis, Wells-Knecht, Kevin J, Dorsey, Bruce D
Published in Journal of medicinal chemistry (12.01.2012)
Published in Journal of medicinal chemistry (12.01.2012)
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Journal Article
Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase
Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Cheng, Mangeng, Ruggeri, Bruce A., Ator, Mark A., Dorsey, Bruce D., Ott, Gregory R.
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
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Journal Article
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors
Tripathy, Rabindranath, Ghose, Arup, Singh, Jasbir, Bacon, Edward R., Angeles, Thelma S., Yang, Shi X., Albom, Mark S., Aimone, Lisa D., Herman, Joseph L., Mallamo, John P.
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
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Journal Article
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
Ott, Gregory R, Wells, Gregory J, Thieu, Tho V, Quail, Matthew R, Lisko, Joseph G, Mesaros, Eugen F, Gingrich, Diane E, Ghose, Arup K, Wan, Weihua, Lu, Lihui, Cheng, Mangeng, Albom, Mark S, Angeles, Thelma S, Huang, Zeqi, Aimone, Lisa D, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D
Published in Journal of medicinal chemistry (22.09.2011)
Published in Journal of medicinal chemistry (22.09.2011)
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Journal Article
Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells
Wan, Weihua, Albom, Mark S., Lu, Lihui, Quail, Matthew R., Becknell, Nadine C., Weinberg, Linda R., Reddy, Dandu R., Holskin, Beverly P., Angeles, Thelma S., Underiner, Ted L., Meyer, Sheryl L., Hudkins, Robert L., Dorsey, Bruce D., Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng
Published in Blood (15.02.2006)
Published in Blood (15.02.2006)
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Journal Article
Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis
Tripathy, Rabindranath, Reiboldt, Alyssa, Messina, Patricia A., Iqbal, Mohamed, Singh, Jasbir, Bacon, Edward R., Angeles, Thelma S., Yang, Shi X., Albom, Mark S., Robinson, Candy, Chang, Hong, Ruggeri, Bruce A., Mallamo, John P.
Published in Bioorganic & medicinal chemistry letters (15.04.2006)
Published in Bioorganic & medicinal chemistry letters (15.04.2006)
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Journal Article
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
Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D
Published in Journal of medicinal chemistry (12.01.2012)
Published in Journal of medicinal chemistry (12.01.2012)
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Journal Article
ALK Mutants in the Kinase Domain Exhibit Altered Kinase Activity and Differential Sensitivity to Small Molecule ALK Inhibitors
Lu, Lihui, Ghose, Arup K, Quail, Matthew R, Albom, Mark S, Durkin, John T, Holskin, Beverly P, Angeles, Thelma S, Meyer, Sheryl L, Ruggeri, Bruce A, Cheng, Mangeng
Published in Biochemistry (Easton) (28.04.2009)
Published in Biochemistry (Easton) (28.04.2009)
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Journal Article
Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group
Tripathy, Rabindranath, McHugh, Robert J., Ghose, Arup K., Ott, Gregory R., Angeles, Thelma S., Albom, Mark S., Huang, Zeck, Aimone, Lisa D., Cheng, Mangeng, Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry letters (15.12.2011)
Published in Bioorganic & medicinal chemistry letters (15.12.2011)
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Journal Article
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone
Tripathy, Rabindranath, Angeles, Thelma S., Yang, Shi X., Mallamo, John P.
Published in Bioorganic & medicinal chemistry (15.06.2008)
Published in Bioorganic & medicinal chemistry (15.06.2008)
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Journal Article
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
Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., Dorsey, Bruce D.
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
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