Thomas H Marsilje

Global Discovery Chemistry; ‡Developmental & Molecular Pathways, §Analytical Sciences, Novartis Institutes for BioMedical Research , Basel 4002, Switzerland.

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April 2014

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

J Med Chem 2013 Jul 26;56(14):5675-90. Epub 2013 Jun 26.

Genomics Institute of the Novartis Research Foundation , 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

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July 2013

High-content micronucleus assay in genotoxicity profiling: initial-stage development and some applications in the investigative/lead-finding studies in drug discovery.

Authors:

Madhu S Mondal Joseph Gabriels Claudia McGinnis Maria Magnifico Thomas H Marsilje Laszlo Urban Alan Collis Dejan Bojanic Scott A Biller Wilfried Frieauff Hans-Joerg Martus Willi Suter Philip Bentley

Toxicol Sci 2010 Nov 14;118(1):71-85. Epub 2010 Jul 14.

Preclinical Safety Profiling, CPC, Novartis Institutes of Biomedical Research, Inc., Cambridge, Massachusetts 02139, USA.

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November 2010

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.

Authors:

Thomas H Marsilje Phil B Alper Wenshuo Lu Daniel Mutnick Pierre-Yves Michellys Yun He Donald S Karanewsky Donald Chow Andrea Gerken Jianmin Lao Min-Ju Kim H Martin Seidel Shin-Shay Tian

Bioorg Med Chem Lett 2008 Oct 26;18(19):5259-62. Epub 2008 Aug 26.

Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.

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October 2008

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

Authors:

Phil B Alper Thomas H Marsilje Daniel Mutnick Wenshuo Lu Arnab Chatterjee Michael J Roberts Yun He Donald S Karanewsky Donald Chow Jianmin Lao Andrea Gerken Tove Tuntland Bo Liu Jonathan Chang Perry Gordon H Martin Seidel Shin-Shay Tian

Bioorg Med Chem Lett 2008 Oct 22;18(19):5255-8. Epub 2008 Aug 22.

Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.

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October 2008

NMR structural studies of interactions of a small, nonpeptidyl Tpo mimic with the thrombopoietin receptor extracellular juxtamembrane and transmembrane domains.

Authors:

Min-Ju Kim Sang Ho Park Stanley J Opella Thomas H Marsilje Pierre-Yves Michellys H Martin Seidel Shin-Shay Tian

J Biol Chem 2007 May 16;282(19):14253-61. Epub 2007 Mar 16.

Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA.

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May 2007

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.

Bioorg Med Chem Lett 2005 Oct;15(19):4174-9

Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.

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October 2005

Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).

Authors:

Thomas H Marsilje Jonathan B Roses Emily F Calderwood Stephen G Stroud Nancy E Forsyth Christopher Blackburn David L Yowe Wenyan Miao Stacey V Drabic Marie D Bohane J Scott Daniels Ping Li Lijun Wu Michael A Patane Christopher F Claiborne

Bioorg Med Chem Lett 2004 Jul;14(14):3721-5

Department of Medicinal Chemistry, Millennium Pharmaceuticals, Inc., Cambridge, MA 02139, USA.

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July 2004

10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.

Authors:

Thomas H Marsilje Michael P Hedrick Joel Desharnais Kevin Capps Ali Tavassoli Yan Zhang Ian A Wilson Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2003 Oct;11(20):4503-9

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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October 2003

Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

Authors:

Thomas H Marsilje Michael P Hedrick Joel Desharnais Ali Tavassoli Yan Zhang Ian A Wilson Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2003 Oct;11(20):4487-501

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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October 2003

Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.

Authors:

Yan Zhang Joel Desharnais Thomas H Marsilje Chenglong Li Michael P Hedrick Lata T Gooljarsingh Ali Tavassoli Stephen J Benkovic Arthur J Olson Dale L Boger Ian A Wilson

Biochemistry 2003 May;42(20):6043-56

Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.

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May 2003

10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway.

Authors:

Thomas H Marsilje Marc A Labroli Michael P Hedrick Qing Jin Joel Desharnais Stephen J Baker Lata T Gooljarsingh Joseph Ramcharan Ali Tavassoli Yan Zhang Ian A Wilson G Peter Beardsley Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2002 Aug;10(8):2739-49

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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August 2002

Publications by authors named "Thomas H Marsilje"

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