Search Results - "Bousquet, Peter F."
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Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor
Published in Molecular cancer therapeutics (01-04-2006)“…ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor…”
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Distinct spatiotemporal pattern of CNS lesions revealed by USPIO-enhanced MRI in MOG-induced EAE rats implicates the involvement of spino-olivocerebellar pathways
Published in Journal of neuroimmunology (25-06-2009)“…Abstract USPIO-enhanced MRI allows non-invasive visualization of mononuclear cell infiltration into CNS lesions in MS and EAE. Herein, we show a distinct…”
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Discovery of N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N‘-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-Aminoindazole-Based Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitor
Published in Journal of medicinal chemistry (05-04-2007)“…In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors as potential anticancer agents, we discovered, through a…”
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Thienopyrimidine Ureas as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors
Published in Journal of medicinal chemistry (22-09-2005)“…A series of novel thienopyrimidine-based receptor tyrosine kinase inhibitors has been discovered. Investigation of structure−activity relationships at the 5-…”
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3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases
Published in Journal of medicinal chemistry (13-03-2008)“…A series of benzoisoxazoles and benzoisothiazoles have been synthesized and evaluated as inhibitors of receptor tyrosine kinases (RTKs). Structure–activity…”
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Thienopyridine urea inhibitors of KDR kinase
Published in Bioorganic & medicinal chemistry letters (01-03-2007)“…The evaluation of KDR kinase inhibitor 2 (IC 50 = 9 nM) and related analogs is reported. A series of substituted thienopyridine ureas was prepared and…”
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1,4-Dihydroindeno[1,2-c]pyrazoles with Acetylenic Side Chains as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors with Low Affinity for the hERG Ion Channel
Published in Journal of medicinal chemistry (03-05-2007)“…The synthesis of a novel series of 1,4-dihydroindeno[1,2-c]pyrazoles with acetylene-type side chains is described. Optimization of those compounds as KDR…”
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Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2- c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-06-2007)“…We report the synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2- c]pyrazoles as multitargeted kinase inhibitors. Initial efforts…”
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Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A series of isothiazolopyrimidines and isoxazolopyrimidines were synthesized and identified as potent RTK inhibitors. SAR studies led to isothiazolopyrimidine…”
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Hit-to-lead optimization of 1,4-dihydroindeno[1,2- c]pyrazoles as a novel class of KDR kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A series of 1,4-dihydroindeno[1,2- c]pyrazoles was evaluated as KDR kinase inhibitors. Hit-to-lead optimization studies led to 19, a lead compound with an…”
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1,4-Dihydroindeno[1,2- c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A series of 1,4-dihydroindeno[1,2- c]pyrazoles with urea-type side chains was identified as potent multitargeted (VEGFR and PDGFR families) receptor tyrosine…”
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Isoindolinone ureas: a novel class of KDR kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (06-09-2004)“…The evaluation of KDR kinase inhibitor 4e (IC 50 7 nM) and related analogs is reported. A series of substituted isoindolinone ureas was prepared and evaluated…”
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Preclinical evaluation of LU 79553: a novel bis-naphthalimide with potent antitumor activity
Published in Cancer research (Chicago, Ill.) (01-03-1995)“…LU 79553 is a novel bis-naphthalimide which is highly cytotoxic in vitro with EC50 (concentration required for 50% inhibition of growth) ranging from 2 x…”
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Effects of cytochalasin B in culture and in vivo on murine Madison 109 lung carcinoma and on B16 melanoma
Published in Cancer research (Chicago, Ill.) (01-03-1990)“…Cytochalasin B (CB), at 100 or at 10 mg/kg single dose s.c. in carboxymethyl-cellulose (2%)/Tween-20 (1%) 24 h after s.c. challenge of B6D2F1 mice with trocar…”
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Benzimidazo[1,2-c]quinazoline dimers as potential antitumor agents
Published in Journal of heterocyclic chemistry (01-05-1997)“…The 6‐substituted benzimidazo[1,2‐c]quinazoline 1 is a lead structure from our DNA intercalator program and is cytotoxic to the human colon cancer tumor line…”
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