B. Dorsey

发表

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Frank Guarnieri, Ted Fujimoto, Zenon Konteatis, 2011, Bioorganic & medicinal chemistry letters.

Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.

W. M. Sanders, Youwei Yan, S. D. Lewis, 2003, Bioorganic & medicinal chemistry letters.

Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2

Jennifer L. Mason, P. Dobrzanski, B. Ruggeri, 2011, The Journal of Immunology.

Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.

J. Vacca, J. Shafer, Z. Chen, 1998, Journal of medicinal chemistry.

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.

G. Pezzoni, B. Ruggeri, J. Mallamo, 2008, Journal of medicinal chemistry.

Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells.

B. Ruggeri, T. Underiner, B. Dorsey, 2006, Blood.

Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein.

A. Lee, S. Majeski, A. Cuconati, 2021, Antiviral research.

Preclinical Profile of AB-423, an Inhibitor of Hepatitis B Virus Pregenomic RNA Encapsidation

Quanxin Long, N. Snead, A. Lee, 2018, Antimicrobial Agents and Chemotherapy.

Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent.

B. Liu, E. Springman, M. Bukhtiyarova, 2011, Journal of medicinal chemistry.

Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2

Jennifer L. Mason, P. Dobrzanski, B. Ruggeri, 2011, The Journal of Immunology.

Is there a scaffolding domain within the structure of the immunosuppressive agent cyclosporin a (CsA)? Studies of the cyclophilin binding domain of CsA

S. Schreiber, R. C. Hawley, N. Anthony, 1988 .

Inhibitor of JAK2 CEP-33779, a Novel, Orally Active, Selective Treatment of Lupus Nephritis in Mice Using Depletion of Autoreactive Plasma Cells and

Mason, B. Ruggeri, D. Gingrich, 2011 .

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).

A. Ghose, P. Dobrzanski, E. Bruckheimer, 2016, Journal of medicinal chemistry.

Synthesis and biological evaluation of sulfonyl acrylonitriles as novel inhibitors to peritoneal carcinomatosis.

S. Kuwada, B. Dorsey, Joseph G Lisko, 2012, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of sulfonyl acrylonitriles as novel inhibitors of cancer metastasis and spread.

J. Shea, B. Ruggeri, C. Scaife, 2015, Journal of medicinal chemistry.

Host Poly(A) Polymerases PAPD5 and PAPD7 Provide Two Layers of Protection That Ensure the Integrity and Stability of Hepatitis B Virus RNA

A. Lee, A. Lam, D. Gotchev, 2021, bioRxiv.

HBsAg mRNA degradation induced by a dihydroquinolizinone compound depends on the HBV posttranscriptional regulatory element

A. Lee, D. Gotchev, R. Rijnbrand, 2018, Antiviral research.

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

J. Vacca, J. Shafer, Z. Chen, 1998, Bioorganic & medicinal chemistry letters.

Efficient synthesis of substituted biaryl anilines and biaryl phenols via a Suzuki cross-coupling reaction

B. Liu, K. Moffett, B. Dorsey, 2005 .

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Tsing-Bau Chen, M. Bock, R. M. Dipardo, 2003, Journal of medicinal chemistry.

L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.

P. Darke, W. Schleif, O. M. Blahy, 1994, Proceedings of the National Academy of Sciences of the United States of America.

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Daniel R McMasters, James C Barrow, W. M. Sanders, 2003, Journal of medicinal chemistry.

Synthesis, antiviral activity, and bioavailability studies of gamma-lactam derived HIV protease inhibitors.

M. Holloway, J. Vacca, R. Hungate, 1994, Bioorganic & medicinal chemistry.

Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

A. Ghose, B. Ruggeri, K. Wells-Knecht, 2012, Journal of medicinal chemistry.

A practical synthesis of 5‐(chloromethyl)furo[2,3‐b]pyridine, a key intermediate for the HIV protease inhibitor, L‐754,394

K. Rossen, J. Hoffman, R. Volante, 1995 .

Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.

A. Ghose, B. Dorsey, T. Angeles, 2011, Bioorganic & medicinal chemistry letters.

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.

A. Ghose, K. Wells-Knecht, H. Breslin, 2012, Journal of medicinal chemistry.

Design of 7-amino-6-chloro-3H-imidazo[4,5-b]pyridine scaffold from 5-chloro-2,4-diaminopyrimidine pharmacophore: identification of potent inhibitors of anaplastic lymphoma kinase

A. Ghose, B. Dorsey, T. Angeles, 2012 .

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.

Jennifer L. Mason, Pawel Dobrzanski, Bruce D. Dorsey, 2012, Journal of medicinal chemistry.

Synthesis of (-)-bertyadionol

M. Malamas, Amos B. Smith, T. Maeda, 1986 .

Evolution of a Synthetic Strategy, Part II: Total Synthesis of (-)-Casbene and (-)-Bertyadionol

Amos B. Smith, B. Dorsey, 1989 .

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.

A. Ghose, B. Ruggeri, D. Gingrich, 2011, Journal of medicinal chemistry.

Synthesis and evaluation of pyridyl analogs of L-735,524: Potent HIV-1 protease inhibitors

P. Anderson, Jiunn H. Lin, P. Darke, 1994 .

L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.

P. Darke, W. Schleif, J. Quintero, 1994, Journal of medicinal chemistry.

A concise and enantioselective synthesis of novel HIV-1 protease transition state mimics

R. Ball, B. Dorsey, Kevin Plzak, 1993 .

Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.

Andrew V. Anzalone, B. Ruggeri, T. Underiner, 2010, ACS medicinal chemistry letters.

Inhibition of HBV replication by N‐hydroxyisoquinolinedione and N‐hydroxypyridinedione ribonuclease H inhibitors

J. Tavis, R. Rijnbrand, M. Sofia, 2019, Antiviral research.

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.

A. Ghose, K. L. Milkiewicz, T. Underiner, 2010, Bioorganic & medicinal chemistry.

P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.

B. Wong, S. D. Lewis, E. A. Lyle, 2011, Bioorganic & medicinal chemistry letters.

Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.

E A Emini, L. Kuo, P. Darke, 2000, Journal of medicinal chemistry.

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

B. Ruggeri, R. Haltiwanger, B. Dorsey, 2015, Bioorganic & medicinal chemistry letters.

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.

K. Wells-Knecht, H. Breslin, B. Dorsey, 2012, Journal of medicinal chemistry.

CEP-28122, a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers

G. Inghirami, B. Ruggeri, D. Gingrich, 2011, Molecular Cancer Therapeutics.

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.

Andrew V. Anzalone, Jason P. Burke, B. Ruggeri, 2011, Bioorganic & medicinal chemistry letters.

CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity

Raffaella Faraoni, Darren E. Insko, P. Dobrzanski, 2012, Molecular Cancer Therapeutics.

Preclinical Development CEP-32496 : A Novel Orally Active BRAFV 600 E Inhibitor with Selective Cellular and In Vivo Antitumor Activity

Raffaella Faraoni, Darren E. Insko, P. Dobrzanski, 2012 .

Anaplastic lymphoma kinase inhibitors as anticancer therapeutics: a patent review

B. Dorsey, G. R. Ott, E. Mesaros, 2014, Expert opinion on therapeutic patents.

The development and pharmacology of proteasome inhibitors for the management and treatment of cancer.

A. Hui, B. Ruggeri, S. Miknyoczki, 2009, Advances in pharmacology.

Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1

Bhavna S. Paratala, R. Rijnbrand, M. Sofia, 2021, Nature Communications.

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis

P. Dobrzanski, B. Ruggeri, D. Gingrich, 2011, Arthritis research & therapy.

Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery

Arup K. Ghose, Bruce D. Dorsey, A. Ghose, 2011, ACS chemical neuroscience.

Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

T. Underiner, B. Dorsey, T. Angeles, 2011, Bioorganic & medicinal chemistry letters.

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

A. Ghose, Brian T. Campbell, Raffaella Faraoni, 2012, Journal of medicinal chemistry.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Brian T. Campbell, Raffaella Faraoni, Andiliy G. Lai, 2011, Bioorganic & Medicinal Chemistry Letters.

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.

Jennifer L. Mason, K. L. Milkiewicz, K. Wells-Knecht, 2011, Bioorganic & Medicinal Chemistry Letters.

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.

Jennifer L. Mason, P. Dobrzanski, K. L. Milkiewicz, 2012, Bioorganic & medicinal chemistry letters.

Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.

H. M. Petrassi, B. Liu, E. Springman, 2010, Bioorganic & medicinal chemistry letters.

Combined inhibition of atypical PKC and histone deacetylase 1 is cooperative in basal cell carcinoma treatment.

A. Butte, M. Sirota, S. Aasi, 2017, JCI insight.

Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.

K. L. Milkiewicz, T. Underiner, B. Dorsey, 2011, Bioorganic & medicinal chemistry letters.

2,7-Disubstituted-pyrrolotriazine kinase inhibitors with an unusually high degree of reactive metabolite formation.

M. Yazdanian, K. Wells-Knecht, D. Gingrich, 2011, Chemical research in toxicology.

Discovery and process synthesis of novel 2,7-pyrrolo[2,1-f][1,2,4]triazines.

A. McLean, H. Breslin, B. Dorsey, 2011, Organic letters.

Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.

K. L. Milkiewicz, S. Miknyoczki, T. Underiner, 2011, Bioorganic & medicinal chemistry.

A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.

T. Halgren, M. Holloway, J. Vacca, 1995, Journal of medicinal chemistry.

An alternate binding site for the P1-P3 group of a class of potent HIV-1 protease inhibitors as a result of concerted structural change in the 80s loop of the protease.

H. B. Schock, L. Kuo, S. Munshi, 2000, Acta crystallographica. Section D, Biological crystallography.

Metabolite-P450 complex formation by methylenedioxyphenyl HIV protease inhibitors in rat and human liver microsomes.

J. Vacca, J. Lin, M. Chiba, 1998, Biochemical pharmacology.

Preclinical antiviral drug combination studies utilizing novel orally bioavailable investigational agents for chronic hepatitis B infection: AB-506, a next generation HBV capsid inhibitor, and AB-452, a HBV RNA destabilizer

K. Mcclintock, S. Majeski, D. Gotchev, 2018 .

471 Screening of Champions predictive TumorGraft platform guides the clinical development of the selective dual BRAF-EGFR inhibitor CEP-32496

E. Bruckheimer, J. Friedman, B. Ruggeri, 2014 .

A. Ghose, Brian T. Campbell, Raffaella Faraoni, 2012, Journal of medicinal chemistry.

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

R. Haltiwanger, B. Dorsey, T. Angeles, 2015, Bioorganic & medicinal chemistry letters.

A. Ghose, K. Wells-Knecht, H. Breslin, 2012, Journal of medicinal chemistry.