Publications by authors named "Steven A Middleton"

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Acute myeloid leukemia patients' clinical response to idasanutlin (RG7388) is associated with pre-treatment MDM2 protein expression in leukemic blasts.
Bernhard Reis, Lori Jukofsky, Gong Chen, Giovanni Martinelli, Hua Zhong, Steven A Middleton

Haematologica· May 2016

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MDM2 antagonist clinical response association with a gene expression signature in acute myeloid leukaemia.
Hua Zhong, Gong Chen, Lori Jukofsky, David Geho, Sung Won Han, Steven A Middleton

Br J Haematol· November 2015

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Pre-clinical evaluation of the MDM2-p53 antagonist RG7388 alone and in combination with chemotherapy in neuroblastoma.
Lindi Chen, Raphaël F Rousseau, Steven A Middleton, Gwen L Nichols, David R Newell

Oncotarget· April 2015

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A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
Tina Morgan Ross, Kathleen Battista, Gilles C Bignan, Doug E Brenneman, Peter J Connolly, Steven A Middleton

Bioorg Med Chem Lett· February 2015

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Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study.
Isabelle Ray-Coquard, Jean-Yves Blay, Antoine Italiano, Axel Le Cesne, Nicolas Penel, Steven A Middleton

Lancet Oncol· November 2012

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Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors.
Anthony W Tolcher, Wells A Messersmith, Stanislaw M Mikulski, Kyriakos P Papadopoulos, Eunice L Kwak, Steven A Middleton

J Clin Oncol· July 2012

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Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
Ronghui Lin, Sigmond G Johnson, Peter J Connolly, Steven K Wetter, Eva Binnun, Steven A Middleton

Bioorg Med Chem Lett· April 2009

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Synthesis, in vitro activities of (2-cyclopropoxyphenyl)piperidine derivatives for alpha 1a and alpha 1d adrenergic receptor inhibitors.
Shengjian Li, George Chiu, Virginia L Pulito, Jingchun Liu, Peter J Connolly, Steven A Middleton

Med Chem· January 2009

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A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.
Terry V Hughes, Guozhang Xu, Steven K Wetter, Peter J Connolly, Stuart L Emanuel, Steven A Middleton

Bioorg Med Chem Lett· September 2008

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7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.
Terry V Hughes, Stuart L Emanuel, Harold R O'Grady, Peter J Connolly, Catherine Rugg, Steven A Middleton

Bioorg Med Chem Lett· September 2008

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4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.
Guozhang Xu, Marta C Abad, Peter J Connolly, Michael P Neeper, Geoffrey T Struble, Steven A Middleton

Bioorg Med Chem Lett· August 2008

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Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.
Guozhang Xu, Lily Lee Searle, Terry V Hughes, Amanda K Beck, Peter J Connolly, Steven A Middleton

Bioorg Med Chem Lett· June 2008

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Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors.
Stuart L Emanuel, Terry V Hughes, Mary Adams, Catherine A Rugg, Angel Fuentes-Pesquera, Steven A Middleton

Mol Pharmacol· February 2008

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(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
George Chiu, Shengjian Li, Peter J Connolly, Virginia Pulito, Jingchun Liu, Steven A Middleton

Bioorg Med Chem Lett· January 2008

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Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
George Chiu, Shengjian Li, Hong Cai, Peter J Connolly, Sean Peng, Steven A Middleton

Bioorg Med Chem Lett· November 2007

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Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Ronghui Lin, Peter J Connolly, Yanhua Lu, George Chiu, Shengjian Li, Steven A Middleton

Bioorg Med Chem Lett· August 2007

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(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
George Chiu, Shengjian Li, Peter J Connolly, Virginia Pulito, Jingchun Liu, Steven A Middleton

Bioorg Med Chem Lett· July 2007

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(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).
George Chiu, Shengjian Li, Peter J Connolly, Virginia Pulito, Jingchun Liu, Steven A Middleton

Bioorg Med Chem Lett· June 2007

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4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.
Terry V Hughes, Stuart L Emanuel, Amanda K Beck, Steven K Wetter, Peter J Connolly, Steven A Middleton

Bioorg Med Chem Lett· June 2007

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Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).
Shenlin Huang, Ronghua Li, Peter J Connolly, Stuart Emanuel, Angel Fuentes-Pesquera, Steven A Middleton

Bioorg Med Chem Lett· April 2007

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Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
Shenlin Huang, Ronghui Lin, Yang Yu, Yanhua Lu, Peter J Connolly, Steven A Middleton

Bioorg Med Chem Lett· March 2007

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1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Shengjian Li, George Chiu, Virginia L Pulito, Jingchun Liu, Peter J Connolly, Steven A Middleton

Bioorg Med Chem Lett· March 2007

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Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
Michael J Orsini, Mark A Klein, Mary Pat Beavers, Peter J Connolly, Steven A Middleton

J Med Chem· February 2007

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Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.
Jennifer A Seamon, Catherine A Rugg, Stuart Emanuel, Anna Maria Calcagno, Suresh V Ambudkar, Steven A Middleton

Mol Cancer Ther· October 2006

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Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
Shenlin Huang, Ronghua Li, Peter J Connolly, Stuart Emanuel, Steven A Middleton

Bioorg Med Chem Lett· September 2006

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