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Steven Middleton

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Ronghui Lin; Sigmond G Johnson; Peter J Connolly; Steven K Wetter; Eva Binnun; Terry V Hughes; William V Murray; Niranjan Pandey; Sandra J Moreno-Mazza; Mary Adams; Angel Fuentes-Pesquera; Steven A Middleton
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
Shengjian Li; George Chiu; Virginia L Pulito; Jingchun Liu; Peter J Connolly; Steven A Middleton
Synthesis, in vitro activities of (2-cyclopropoxyphenyl)piperidine derivatives for alpha 1a and alpha 1d adrenergic receptor inhibitors.
Terry V Hughes; Stuart Emanuel; Harold R O'Grady; Peter J Connolly; Catherine Rugg; Angel Fuentes-Pesquera; Prabha Karnachi; Richard Alexander; Steven A Middleton
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.

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All Publications

2009: Ronghui Lin; Sigmond G Johnson; Peter J Connolly; Steven K Wetter; Eva Binnun; Terry V Hughes; William V Murray; Niranjan Pandey; Sandra J Moreno-Mazza; Mary Adams; Angel Fuentes-Pesquera; Steven A Middleton
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(8):2333-7.
2009: Shengjian Li; George Chiu; Virginia L Pulito; Jingchun Liu; Peter J Connolly; Steven A Middleton
Synthesis, in vitro activities of (2-cyclopropoxyphenyl)piperidine derivatives for alpha 1a and alpha 1d adrenergic receptor inhibitors.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2009;5(1):15-22.
2008: Terry V Hughes; Stuart Emanuel; Harold R O'Grady; Peter J Connolly; Catherine Rugg; Angel Fuentes-Pesquera; Prabha Karnachi; Richard Alexander; Steven A Middleton
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.
Bioorganic & medicinal chemistry letters 2008;18(18):5130-3.
2008: Terry V Hughes; Guozhang Xu; Steven K Wetter; Peter J Connolly; Stuart Emanuel; Prabha Karnachi; Scott R Pollack; Niranjan Pandey; Mary Adams; Sandra Moreno-Mazza; Steven A Middleton; Lee M Greenberger
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.
Bioorganic & medicinal chemistry letters 2008;18(17):4896-9.
2008: Guozhang Xu; Marta C Abad; Peter J Connolly; Michael P Neeper; Geoffrey T Struble; Barry A Springer; Stuart Emanuel; Niranjan Pandey; Robert H Gruninger; Mary Adams; Sandra Moreno-Mazza; Angel Fuentes-Pesquera; Steven A Middleton
4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(16):4615-9.
2008: Guozhang Xu; Lily Lee Searle; Terry V Hughes; Amanda K Beck; Peter J Connolly; Marta C Abad; Michael P Neeper; Geoffrey T Struble; Barry A Springer; Stuart Emanuel; Robert H Gruninger; Niranjan Pandey; Mary Adams; Sandra Moreno-Mazza; Angel Fuentes-Pesquera; Steven A Middleton; Lee M Greenberger
Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.
Bioorganic & medicinal chemistry letters 2008;18(12):3495-9.
2008: Stuart Emanuel; Terry V Hughes; Mary Adams; Catherine A Rugg; Angel Fuentes-Pesquera; Peter J Connolly; Niranjan Pandey; Sandra Moreno-Mazza; Jeannene Butler; Virna Borowski; Steven A Middleton; Robert H Gruninger; Jennifer R Story; Cheryl Napier; Beth Hollister; Lee M Greenberger
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.
Molecular pharmacology 2008;73(2):338-48.
2008: George Chiu; Shengjian Li; Peter J Connolly; Virginia L Pulito; Jingchun Liu; Steven A Middleton
(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorganic & medicinal chemistry letters 2008;18(2):640-4.
2007: George Chiu; Shengjian Li; Hong Cai; Peter J Connolly; Sean Peng; Kathe Stauber; Virginia L Pulito; Jingchun Liu; Steven A Middleton
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).
Bioorganic & medicinal chemistry letters 2007;17(22):6123-8.
2007: Ronghui Lin; Peter J Connolly; Yanhua Lu; George Chiu; Shengjian Li; Yang Yu; Shenlin Huang; Xun Li; Stuart Emanuel; Steven A Middleton; Robert H Gruninger; Mary Adams; Angel Fuentes-Pesquera; Lee M Greenberger
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Bioorganic & medicinal chemistry letters 2007;17(15):4297-302.
2007: George Chiu; Shengjian Li; Peter J Connolly; Virginia L Pulito; Jingchun Liu; Steven A Middleton
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorganic & medicinal chemistry letters 2007;17(14):3930-4.
2007: Terry V Hughes; Stuart Emanuel; Amanda K Beck; Steven K Wetter; Peter J Connolly; Prabha Karnachi; Michael Reuman; Jabed Seraj; Angel Fuentes-Pesquera; Robert H Gruninger; Steven A Middleton; Ronghui Lin; Jeremy M Davis; David F C Moffat
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2007;17(12):3266-70.
2007: George Chiu; Shengjian Li; Peter J Connolly; Virginia L Pulito; Jingchun Liu; Steven A Middleton
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).
Bioorganic & medicinal chemistry letters 2007;17(12):3292-7.
2007: Shenlin Huang; Ronghua Li; Peter J Connolly; Stuart Emanuel; Angel Fuentes-Pesquera; Mary Adams; Robert H Gruninger; Jabed Seraj; Steven A Middleton; Jeremy M Davis; David F C Moffat
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).
Bioorganic & medicinal chemistry letters 2007;17(8):2179-83.
2007: Shengjian Li; George Chiu; Virginia L Pulito; Jingchun Liu; Peter J Connolly; Steven A Middleton
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Bioorganic & medicinal chemistry letters 2007;17(6):1646-50.
2007: Shenlin Huang; Ronghui Lin; Yang Yu; Yanhua Lu; Peter J Connolly; George Chiu; Shengjian Li; Stuart Emanuel; Steven A Middleton
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
Bioorganic & medicinal chemistry letters 2007;17(5):1243-5.
2007: Michael J Orsini; Mark A Klein; Mary Pat Beavers; Peter J Connolly; Steven A Middleton; Kevin H Mayo
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
Journal of medicinal chemistry 2007;50(3):462-71.
2006: Jennifer A Seamon; Catherine A Rugg; Stuart Emanuel; Anna Maria Calcagno; Suresh V Ambudkar; Steven A Middleton; Jeannene Butler; Virna Borowski; Lee M Greenberger
Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.
Molecular cancer therapeutics 2006;5(10):2459-67.
2006: Shenlin Huang; Ronghua Li; Peter J Connolly; Stuart Emanuel; Steven A Middleton
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(18):4818-21.
2006: Shenlin Huang; Peter J Connolly; Ronghui Lin; Stuart Emanuel; Steven A Middleton
Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.
Bioorganic & medicinal chemistry letters 2006;16(14):3639-41.
2006: Gilles C Bignan; Kathleen Battista; Peter J Connolly; Michael J Orsini; Jingchun Liu; Steven A Middleton; Allen B Reitz
3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Bioorganic & medicinal chemistry letters 2006;16(13):3524-8.
2005: Chih Y Ho; Donald W Ludovici; Umar S M Maharoof; Jay Mei; Jan L Sechler; Robert W Tuman; Eric D Strobel; Laura Andraka; Hwa-Kwo Yen; Gregory C Leo; Jian Li; Harold Almond; Hong Lu; Ann DeVine; Rose Tominovich; Judith Baker; Stuart Emanuel; Robert H Gruninger; Steven A Middleton; Dana L Johnson; Robert Anthony Galemmo
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
Journal of medicinal chemistry 2005;48(26):8163-73.
2005: Gilles C Bignan; Kathleen Battista; Peter J Connolly; Michael J Orsini; Jingchun Liu; Steven A Middleton; Allen B Reitz
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Bioorganic & medicinal chemistry letters 2005;15(22):5022-6.
2005: Alfonzo D Jordan; Michael J Orsini; Steven A Middleton; Peter J Connolly; Douglas E Brenneman; Kevin Pan; Allen B Reitz
8-(Heteroaryl)phenalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as opioid receptor modulators.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2005;1(6):601-10.
2005: Stuart Emanuel; Catherine A Rugg; Robert H Gruninger; Ronghui Lin; Angel Fuentes-Pesquera; Peter J Connolly; Steven K Wetter; Beth Hollister; Walter W Kruger; Cheryl Napier; Linda Jolliffe; Steven A Middleton
The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.
Cancer research 2005;65(19):9038-46.
2005: Gee-Hong Kuo; Catherine Prouty; Aihua Wang; Stuart Emanuel; Alan DeAngelis; Yan Zhang; Fengbin Song; Lawrence Beall; Peter J Connolly; Prabha Karnachi; Xin Chen; Robert H Gruninger; Jan L Sechler; Angel Fuentes-Pesquera; Steven A Middleton; Linda Jolliffe; William V Murray
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Journal of medicinal chemistry 2005;48(15):4892-909.
2005: Gee-Hong Kuo; Alan DeAngelis; Stuart Emanuel; Aihua Wang; Yan Zhang; Peter J Connolly; Xin Chen; Robert H Gruninger; Catherine A Rugg; Angel Fuentes-Pesquera; Steven A Middleton; Linda Jolliffe; William V Murray
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
Journal of medicinal chemistry 2005;48(14):4535-46.
2005: Ronghui Lin; Peter J Connolly; Shenlin Huang; Steven K Wetter; Yanhua Lu; William V Murray; Stuart Emanuel; Robert H Gruninger; Angel Fuentes-Pesquera; Catherine A Rugg; Steven A Middleton; Linda Jolliffe
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
Journal of medicinal chemistry 2005;48(13):4208-11.
2005: Ronghui Lin; Yanhua Lu; Steven K Wetter; Peter J Connolly; Ignatius Turchi; William V Murray; Stuart Emanuel; Robert H Gruninger; Angel Fuentes-Pesquera; Mary Adams; Niranjan Pandey; Sandra Moreno-Mazza; Steven A Middleton; Linda Jolliffe
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2005;15(9):2221-4.
2005: Gee-Hong Kuo; Aihua Wang; Stuart Emanuel; Alan DeAngelis; Rui Zhang; Peter J Connolly; William V Murray; Robert H Gruninger; Jan L Sechler; Angel Fuentes-Pesquera; Dana Johnson; Steven A Middleton; Linda Jolliffe; Xin Chen
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.
Journal of medicinal chemistry 2005;48(6):1886-900.
2005: Michael J Orsini; Irina Nesmelova; Helen C Young; Balazs Hargittai; Mary Pat Beavers; Jingchun Liu; Peter J Connolly; Steven A Middleton; Kevin H Mayo
The nociceptin pharmacophore site for opioid receptor binding derived from the NMR structure and bioactivity relationships.
The Journal of biological chemistry 2005;280(9):8134-42.
2004: Stuart Emanuel; Robert H Gruninger; Angel Fuentes-Pesquera; Peter J Connolly; Jennifer A Seamon; Susan Hazel; Rose Tominovich; Beth Hollister; Cheryl Napier; Michael R D'Andrea; Michael Reuman; Gilles C Bignan; Robert W Tuman; Dana Johnson; David Moffatt; Mark Batchelor; Anne Foley; James O'Connell; Rodger Allen; Martin Perry; Linda Jolliffe; Steven A Middleton
A vascular endothelial growth factor receptor-2 kinase inhibitor potentiates the activity of the conventional chemotherapeutic agents paclitaxel and doxorubicin in tumor xenograft models.
Molecular pharmacology 2004;66(3):635-47.
2003: Gee-Hong Kuo; Catherine Prouty; Alan DeAngelis; Lan Shen; David J O'Neill; Chandra Shah; Peter J Connolly; William V Murray; Bruce R Conway; Peter Cheung; Lori Westover; Jun Z Xu; Richard Look; Keith T Demarest; Stuart Emanuel; Steven A Middleton; Linda Jolliffe; Mary Pat Beavers; Xin Chen
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.
Journal of medicinal chemistry 2003;46(19):4021-31.
1999: Steven A Middleton; FP Barbone; Dana L Johnson; Robin Thurmond; Y You; FJ McMahon; R Jin; O Livnah; Jennifer Tullai; Francis X Farrell; Mark A Goldsmith; Ian A Wilson; Linda Jolliffe
Shared and unique determinants of the erythropoietin (EPO) receptor are important for binding EPO and EPO mimetic peptide.
The Journal of biological chemistry 1999;274(20):14163-9.
1999: O Livnah; Enrico STURA; Steven A Middleton; Dana L Johnson; Linda Jolliffe; Ian A Wilson
Crystallographic evidence for preformed dimers of erythropoietin receptor before ligand activation.
Science (New York, N.Y.) 1999;283(5404):987-90.
1999: FP Barbone; Dana L Johnson; Francis X Farrell; A Collins; Steven A Middleton; FJ McMahon; Jennifer Tullai; Linda Jolliffe
New epoetin molecules and novel therapeutic approaches.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 1999;14 Suppl 2():80-4.
1998: Dana L Johnson; Francis X Farrell; FP Barbone; FJ McMahon; Jennifer Tullai; K Hoey; O Livnah; NC Wrighton; Steven A Middleton; DA Loughney; Enrico STURA; William J Dower; LS Mulcahy; Ian A Wilson; Linda Jolliffe
Identification of a 13 amino acid peptide mimetic of erythropoietin and description of amino acids critical for the mimetic activity of EMP1.
Biochemistry 1998;37(11):3699-710.
1997: FP Barbone; Steven A Middleton; Dana L Johnson; FJ McMahon; Jennifer Tullai; Robert H Gruninger; A E Schilling; Linda Jolliffe; LS Mulcahy
Mutagenesis studies of the human erythropoietin receptor. Establishment of structure-function relationships.
The Journal of biological chemistry 1997;272(8):4985-92.
1996: O Livnah; Enrico STURA; Dana L Johnson; Steven A Middleton; LS Mulcahy; N C Wrighton; William J Dower; Linda Jolliffe; Ian A Wilson
Functional mimicry of a protein hormone by a peptide agonist: the EPO receptor complex at 2.8 A.
Science (New York, N.Y.) 1996;273(5274):464-71.
1996: Steven A Middleton; Dana L Johnson; R Jin; FJ McMahon; A Collins; Jennifer Tullai; R H Gruninger; Linda Jolliffe; LS Mulcahy
Identification of a critical ligand binding determinant of the human erythropoietin receptor. Evidence for common ligand binding motifs in the cytokine receptor family.
The Journal of biological chemistry 1996;271(24):14045-54.
1996: Dana L Johnson; Steven A Middleton; F McMahon; FP Barbone; D Kroon; Erich I Tsao; W H Lee; LS Mulcahy; Linda Jolliffe
Refolding, purification, and characterization of human erythropoietin binding protein produced in Escherichia coli.
Protein expression and purification 1996;7(1):104-13.
1995: Linda Jolliffe; Steven A Middleton; FP Barbone; Dana L Johnson; FJ McMahon; W H Lee; R H Gruninger; LS Mulcahy
Erythropoietin receptor: application in drug development.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 1995;10 Suppl 2():28-34.