D. Shen

发表

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase in

Ping Chen, A. Doweyko, Derek J. Norris, 2006, Journal of medicinal chemistry.

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.

Gulzar Ahmed, Arthur M Doweyko, Axel Metzger, 2005, Journal of medicinal chemistry.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2011, Bioorganic & medicinal chemistry letters.

5-amino-pyrazoles as potent and selective p38α inhibitors.

A. Doweyko, R. Moquin, K. McIntyre, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

A. Doweyko, R. Moquin, K. McIntyre, 2008, Bioorganic & medicinal chemistry letters.

Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.

Michael A. Galella, D. Shen, C. Weigelt, 2020, Bioorganic & medicinal chemistry letters.

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials.

Michael G. Yang, K. McIntyre, D. Shen, 2019, Journal of medicinal chemistry.

High-throughput high-content imaging assays for identification and characterization of selective AXL pathway inhibitors.

K. Constantine, D. Shen, M. Witmer, 2014, Assay and drug development technologies.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

A. Doweyko, James Lin, J. Wityak, 2010, Journal of medicinal chemistry.

Integrating High-Content Analysis into a Multiplexed Screening Approach to Identify and Characterize GPCR Agonists

D. Shen, M. Banks, John Watson, 2014, Journal of biomolecular screening.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Michael A. Galella, K. McIntyre, D. Shen, 2016, Journal of medicinal chemistry.

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Ping Chen, A. Doweyko, R. Moquin, 2003, Bioorganic & medicinal chemistry letters.

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

A. Doweyko, R. Moquin, James Lin, 2003, Bioorganic & medicinal chemistry letters.

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.

A. Doweyko, S. Spergel, R. Moquin, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.

Ping Chen, Derek J. Norris, Henry H. Gu, 2002, Bioorganic & medicinal chemistry letters.

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.

Michael G. Yang, K. McIntyre, D. Shen, 2016, Journal of medicinal chemistry.

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Michael A. Galella, D. Shuster, D. Shen, 2019, ACS medicinal chemistry letters.

Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

J. Y. Roberge, Ping Chen, A. Doweyko, 2002, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

John Dodd, John S Tokarski, Arthur M Doweyko, 2008, Journal of medicinal chemistry.

BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.

Derek J. Norris, D. Shen, G. Trainor, 2015, Bioorganic & medicinal chemistry letters.

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Bioorganic & medicinal chemistry letters.

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Wei Li, Gulzar Ahmed, John Dodd, 2004, Journal of medicinal chemistry.

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.

K. McIntyre, D. Shuster, D. Shen, 2016, Journal of medicinal chemistry.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

S. Spergel, R. Moquin, K. McIntyre, 2016, Journal of medicinal chemistry.

Identification of potent tricyclic prodrug S1P1 receptor modulators.

K. McIntyre, D. Shen, A. Mathur, 2017, MedChemComm.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

S. Spergel, K. McIntyre, D. Shuster, 2016, Bioorganic & medicinal chemistry letters.

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

K. McIntyre, D. Shen, J. Barrish, 2016, ACS medicinal chemistry letters.

Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.

Derek J. Norris, D. Shen, G. Trainor, 2015, ACS medicinal chemistry letters.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Michael A. Galella, D. Shen, J. Barrish, 2018, Bioorganic & medicinal chemistry letters.

Aryl Ether-Derived Sphingosine-1-Phosphate Receptor (S1P1) Modulators: Optimization of the PK, PD, and Safety Profiles.

Michael G. Yang, K. McIntyre, D. Shen, 2020, ACS medicinal chemistry letters.

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.