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Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530

by Green, Tim P., Fennell, Mike, Whittaker, Robin, Curwen, Jon, Jacobs, Vivien, Allen, Jack, Logie, Armelle, Hargreaves, Judith, Hickinson, D. Mark, Wilkinson, Robert W., Elvin, Paul, Boyer, Brigitte, Carragher, Neil, Plé, Patrick A., Bermingham, Alun, Holdgate, Geoffrey A., Ward, Walter H.J., Hennequin, Laurent F., Davies, Barry R., Costello, Gerard F.
Published in Molecular oncology (01.06.2009)

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N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a Novel, Highly Selective, Orally Available, Dual-Specific c-Src/Abl Kinase Inhibitor

N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a Novel, Highly Selective, Orally Available, Dual-Specific c-Src/Abl Kinase Inhibitor

by Hennequin, Laurent F, Allen, Jack, Breed, Jason, Curwen, Jon, Fennell, Michael, Green, Tim P, Lambert-van der Brempt, Christine, Morgentin, Rémy, Norman, Richard A, Olivier, Annie, Otterbein, Ludovic, Plé, Patrick A, Warin, Nicolas, Costello, Gerard
Published in Journal of medicinal chemistry (02.11.2006)

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Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

by Degorce, Sébastien L, Bailey, Andrew, Callis, Rowena, De Savi, Chris, Ducray, Richard, Lamont, Gillian, MacFaul, Philip, Maudet, Mickael, Martin, Scott, Morgentin, Rémy, Norman, Richard A, Peru, Aurélien, Pink, Jennifer H, Plé, Patrick A, Roberts, Bryan, Scott, James S
Published in Journal of medicinal chemistry (23.04.2015)

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Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases

Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases

by Plé, Patrick A., Jung, Frédéric, Ashton, Sue, Hennequin, Laurent, Laine, Romuald, Morgentin, Rémy, Pasquet, Georges, Taylor, Sian
Published in Bioorganic & medicinal chemistry letters (01.01.2012)

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New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors

New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors

by Barlaam, Bernard, Fennell, Mike, Germain, Hervé, Green, Tim, Hennequin, Laurent, Morgentin, Rémy, Olivier, Annie, Plé, Patrick, Vautier, Michel, Costello, Gerard
Published in Bioorganic & medicinal chemistry letters (15.12.2005)

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Discovery of a New Class of Anilinoquinazoline Inhibitors with High Affinity and Specificity for the Tyrosine Kinase Domain of c-Src

Discovery of a New Class of Anilinoquinazoline Inhibitors with High Affinity and Specificity for the Tyrosine Kinase Domain of c-Src

by Plé, Patrick A, Green, Tim P, Hennequin, Laurent F, Curwen, Jon, Fennell, Michael, Allen, Jack, Lambert-van der Brempt, Christine, Costello, Gerard
Published in Journal of medicinal chemistry (12.02.2004)

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Novel 4-Anilinoquinazolines with C-7 Basic Side Chains: Design and Structure Activity Relationship of a Series of Potent, Orally Active, VEGF Receptor Tyrosine Kinase Inhibitors

Novel 4-Anilinoquinazolines with C-7 Basic Side Chains: Design and Structure Activity Relationship of a Series of Potent, Orally Active, VEGF Receptor Tyrosine Kinase Inhibitors

by Hennequin, Laurent F, Stokes, Elaine S. E, Thomas, Andrew P, Johnstone, Craig, Plé, Patrick A, Ogilvie, Donald J, Dukes, Michael, Wedge, Stephen R, Kendrew, Jane, Curwen, Jon O
Published in Journal of medicinal chemistry (14.03.2002)

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Correction to Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Correction to Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

by Degorce, Sébastien L, Bailey, Andrew, Callis, Rowena, De Savi, Chris, Ducray, Richard, Lamont, Gillian, MacFaul, Philip, Maudet, Mickael, Martin, Scott, Morgentin, Rémy, Norman, Richard A, Peru, Aurélien, Pink, Jennifer H, Plé, Patrick A, Roberts, Bryan, Scott, James S
Published in Journal of medicinal chemistry (14.04.2016)

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Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases

Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases

by Plé, Patrick A., Jung, Frédéric, Ashton, Sue, Hennequin, Laurent, Laine, Romuald, Lambert-van der Brempt, Christine, Morgentin, Rémy, Pasquet, Georges, Taylor, Sian
Published in Bioorganic & medicinal chemistry letters (01.05.2012)

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Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

by Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Giordanetto, Fabrizio, Green, Stephen, Inghardt, Tord, Hennequin, Laurent, Hancox, Urs, Lambert-van der Brempt, Christine, Morgentin, Rémy, Pass, Sarah, Plé, Patrick, Saleh, Twana, Ward, Lara
Published in Bioorganic & medicinal chemistry letters (15.08.2014)

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Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

by Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Ellston, Rebecca, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Plé, Patrick, Ward, Lara, Warin, Nicolas
Published in Bioorganic & medicinal chemistry letters (01.05.2017)

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Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

by Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Péru, Aurélien, Plé, Patrick, Saleh, Twana, Ward, Lara, Warin, Nicolas
Published in Bioorganic & medicinal chemistry letters (01.05.2016)

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Discovery of (R)-8-(1-(3,5-Difluorophenylamino)ethyl)-N,N-dimethy12-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3K beta and P13K delta for the Treatment of PTEN-Deficient Cancers

Discovery of (R)-8-(1-(3,5-Difluorophenylamino)ethyl)-N,N-dimethy12-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3K beta and P13K delta for the Treatment of PTEN-Deficient Cancers

by Barlaam, Bernard, Cosulich, Sabina, Degorce, Sebastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickael, Morgentin, Remy, Pasquet, Marie-Jeanne, Peru, Aurelien, Ple, Patrick, Saleh, Twana, Vautier, Michel, Walker, Mike, Ward, Lara, Warin, Nicolas
Published in Journal of medicinal chemistry (22.01.2015)

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Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series

by Barlaam, Bernard, Ducray, Richard, Brempt, Christine Lambert-van der, Plé, Patrick, Bardelle, Catherine, Brooks, Nigel, Coleman, Tanya, Cross, Darren, Kettle, Jason G., Read, Jon
Published in Bioorganic & medicinal chemistry letters (15.04.2011)

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Journal Article

Discovery of (R)‑8-(1-(3,5-Difluorophenylamino)ethyl)‑N,N‑dimethyl-2-morpholino-4-oxo‑4H‑chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

Discovery of (R)‑8-(1-(3,5-Difluorophenylamino)ethyl)‑N,N‑dimethyl-2-morpholino-4-oxo‑4H‑chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

by Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Pasquet, Marie-Jeanne, Péru, Aurélien, Plé, Patrick, Saleh, Twana, Vautier, Michel, Walker, Mike, Ward, Lara, Warin, Nicolas
Published in Journal of medicinal chemistry (22.01.2015)

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Strategic studies in the syntheses of novel 6,7-substituted quinolones and 7- or 6-substituted 1,6- and 1,7-naphthyridones

Strategic studies in the syntheses of novel 6,7-substituted quinolones and 7- or 6-substituted 1,6- and 1,7-naphthyridones

by Morgentin, Rémy, Pasquet, Georges, Boutron, Pascal, Jung, Frédéric, Lamorlette, Maryannick, Maudet, Mickaël, Plé, Patrick
Published in Tetrahedron (17.03.2008)

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An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate

An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate

by Morgentin, Rémy, Jung, Frédéric, Lamorlette, Maryannick, Maudet, Mickaël, Ménard, Morgan, Plé, Patrick, Pasquet, Georges, Renaud, Fabrice
Published in Tetrahedron (24.01.2009)

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Design and Structure−Activity Relationship of a New Class of Potent VEGF Receptor Tyrosine Kinase Inhibitors

Design and Structure−Activity Relationship of a New Class of Potent VEGF Receptor Tyrosine Kinase Inhibitors

by Hennequin, Laurent F, Thomas, Andrew P, Johnstone, Craig, Stokes, Elaine S. E, Plé, Patrick A, Lohmann, Jean-Jacques M, Ogilvie, Donald J, Dukes, Mike, Wedge, Steve R, Curwen, Jon O, Kendrew, Jane, Lambert-van der Brempt, Christine
Published in Journal of medicinal chemistry (30.12.1999)

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Investigation of (E)-344-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Investigation of (E)-344-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

by Degorce, Sebastien L., Bailey, Andrew, Callis, Rowena, De Savi, Chris, Ducray, Richard, Lamontt, Gillian, MacFaul, Philip, Maudet, Mickael, Martin, Scott, Morgentin, Remy, Norman, Richard A., Peru, Aurelien, Pink, Jennifer H., Ple, Patrick A., Roberts, Bryan, Scott, James S.
Published in Journal of medicinal chemistry (23.04.2015)

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Two-Directional Approach for the Rapid Synthesis of 2,4-Bis-Aminoaryl Pyridine Derivatives

Two-Directional Approach for the Rapid Synthesis of 2,4-Bis-Aminoaryl Pyridine Derivatives

by Morgentin, Rémy, Barlaam, Bernard, Foote, Kevin, Hassall, Lorraine, Hawkins, Janet, Jones, Clifford D., Le Griffon, Antoine, Peru, Aurelien, Plé, Patrick
Published in Synthetic communications (01.01.2012)

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