Search Results - "Volpi, Daniele"
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A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity
Published in Nature chemical biology (01-06-2008)“…Cdc7 is an essential kinase that promotes DNA replication by activating origins of replication. Here, we characterized the potent Cdc7 inhibitor PHA-767491 ( 1…”
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Identification of 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors
Published in Journal of medicinal chemistry (13-05-2010)“…Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is…”
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Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding
Published in Journal of medicinal chemistry (28-10-2010)“…Cdc7 serine/threonine kinase is a key regulator of DNA synthesis in eukaryotic organisms. Cdc7 inhibition through siRNA or prototype small molecules causes p53…”
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Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potential Antitumor Agents. 1. Synthesis and Structure–Activity Relationships
Published in Journal of medicinal chemistry (14-02-2008)“…Cdc7 kinase is an essential protein that promotes DNA replication in eukaryotic organisms. Genetic evidence indicates that Cdc7 inhibition can cause selective…”
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Optimization of 6,6-dimethyl pyrrolo[3,4- c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing
Published in Bioorganic & medicinal chemistry (01-03-2010)“…We describe the synthesis of compounds with interesting biochemical and cellular characteristics. Optimization of the physico-chemical properties led to the…”
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Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships
Published in Journal of medicinal chemistry (23-07-2009)“…Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective…”
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First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery
Published in Journal of medicinal chemistry (22-01-2009)“…Cdc7 kinase is a key regulator of the S-phase of the cell cycle, known to promote the activation of DNA replication origins in eukaryotic organisms. Cdc7…”
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Online tracking of interventional devices for endovascular aortic repair
Published in International journal for computer assisted radiology and surgery (01-06-2015)“…Purpose The continuous integration of innovative imaging modalities into conventional vascular surgery rooms has led to an urgent need for computer assistance…”
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Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors
Published in Journal of medicinal chemistry (11-03-2010)“…Abnormal proliferation mediated by disruption of the mechanisms that keep the cell cycle under control is a hallmark of virtually all cancer cells. Compounds…”
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Thieno[3,2- c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity
Published in Bioorganic & medicinal chemistry (01-10-2010)“…In this paper we report on the optimization of the thieno[3,2- c]pyrazole series as inhibitors of the Aurora kinases to give a promising lead compound endowed…”
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Abstract DD01-01: NMS-1116354: More than an inhibitor of Cdc 7 kinase in S-phase
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract Most of the widely used anticancer drugs target the elongation step of DNA synthesis, either directly, for example by restricting the pool of dNTPs or…”
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Abstract C202: Targeting the mitotic checkpoint for cancer therapy with NMS-P715, a novel MPS1 kinase inhibitor
Published in Molecular cancer therapeutics (10-12-2009)“…Abstract The Spindle Assembly Checkpoint (SAC) is a mitotic mechanism specifically required for proper chromosomal segregation ensuring that cells do not…”
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Cell Division Cycle 7 Kinase Inhibitors: 1 H -Pyrrolo[2,3- b ]pyridines, Synthesis and Structure−Activity Relationships
Published in Journal of medicinal chemistry (23-07-2009)Get full text
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First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery
Published in Journal of medicinal chemistry (26-02-2009)Get full text
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Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3
Published in Bioorganic & medicinal chemistry letters (09-02-2004)“…We describe the synthesis of a series of low molecular weight inhibitors of the αvβ3 integrin obtained by modifying a high-throughput screening hit with…”
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Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3
Published in Bioorganic & medicinal chemistry letters (09-02-2004)“…We describe the synthesis of a series of low molecular weight inhibitors of the alphavbeta3 integrin obtained by modifying a high-throughput screening hit with…”
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Endothelin-1-selective binding sites are downregulated by transforming growth factor-beta and upregulated by basic fibroblast growth factor in a vascular smooth muscle-derived cell line
Published in Journal of cardiovascular pharmacology (01-06-1994)“…Endothelins (ETs) elicit in vivo and in vitro a potent vasoconstrictor activity after binding to high-affinity receptors on vascular smooth muscle cells…”
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Agents Combining Thromboxane Receptor Antagonism with Thromboxane Synthase Inhibition: [[[2-(1H-Imidazol-1-yl)ethylidene]amino]oxy]alkanoic Acids
Published in Journal of medicinal chemistry (01-10-1994)“…A new class of compounds combining thromboxane-A2 (TxA2) receptor antagonism and thromboxane synthase inhibition is described. A first series of (E)- and…”
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Inactivation of endothelin by polymorphonuclear leukocyte-derived lytic enzymes
Published in Blood (15-11-1991)“…Cultured bovine aortic endothelial cells (BAEC) released endothelin-1 (ET-1) in the culture medium in a time-dependent fashion. Coincubation of fMLP-activated…”
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