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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (13), p.3741-3748

2013

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Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach

ACS medicinal chemistry letters, 2017-03, Vol.8 (3), p.338-343

2017

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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

ACS medicinal chemistry letters, 2016-08, Vol.7 (8), p.735-740

2016

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The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells

Cancer research (Chicago, Ill.), 2007-07, Vol.67 (14), p.6956-6964

2007

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Tyrosine kinase inhibitors: From rational design to clinical trials

Medicinal research reviews, 2001-11, Vol.21 (6), p.499-512

2001

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Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models

Molecular cancer therapeutics, 2007-09, Vol.6 (9), p.2496-2504

2007

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Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials

Molecular cancer therapeutics, 2014-05, Vol.13 (5), p.1117-1129

2014

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Selective GRB2 SH2 inhibitors as anti‐Ras therapy

International journal of cancer, 1999-10, Vol.83 (2), p.235-241

1999

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Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy

Biochemistry (Easton), 2018-09, Vol.57 (38), p.5576-5590

2018

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The Total Synthesis and Biological Assessment of trans-Epothilone A

Helvetica chimica acta, 2002-11, Vol.85 (11), p.4086-4110

2002

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Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain

Journal of medicinal chemistry, 1998-08, Vol.41 (18), p.3442-3449

1998

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Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

Blood, 2017-12, Vol.130, p.1383-1383

2017

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Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8345-8379

2022

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A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and In vitro anti‐proliferative as well as In vivo anti‐tumor activity

International journal of cancer, 1989-05, Vol.43 (5), p.851-856

1989

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Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility

The Journal of biological chemistry, 1999-08, Vol.274 (33), p.23311-23315

1999

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AEE788: A dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity

Cancer research (Chicago, Ill.), 2004-07, Vol.64 (14), p.4931-4941

2004

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Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands

Journal of molecular biology, 1998-06, Vol.279 (4), p.1013-1022

1998

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Recent developments in the chemistry and biology of epothilones

ARKIVOC, 2006-09, Vol.2006 (8), p.131-141

2006

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Potent Antagonists of the SH2 Domain of Grb2: Optimization of the X+1 Position of 3-Amino-Z-Tyr(PO3H2)-X+1-Asn-NH2

Journal of medicinal chemistry, 1998-05, Vol.41 (11), p.1741-1744

1998

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Entry into a new class of protein kinase inhibitors by pseudo ring design

Bioorganic & medicinal chemistry, 2008-02, Vol.18 (3), p.897-900

2008

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Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3569-3574

2015

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Structural basis for specificity of GRB2-SH2 revealed by a novel ligand binding mode

Nature structural biology, 1996-07, Vol.3 (7), p.586-589

1996

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Protein kinases as targets for anticancer agents: from inhibitors to useful drugs

Pharmacology & therapeutics (Oxford), 2002-02, Vol.93 (2), p.79-98

2002

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Epothilones and Their Analogs – Potential New Weapons in the Fight Against Cancer

Chimia, 2000-01, Vol.54 (11), p.612

2000

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Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (19), p.4729-4734

2016

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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells

Tyrosine kinase inhibitors: From rational design to clinical trials

Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models

Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials

Selective GRB2 SH2 inhibitors as anti‐Ras therapy

Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy

The Total Synthesis and Biological Assessment of trans-Epothilone A

Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain

Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor

A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and In vitro anti‐proliferative as well as In vivo anti‐tumor activity

Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility

AEE788: A dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity

Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands

Recent developments in the chemistry and biology of epothilones

Potent Antagonists of the SH2 Domain of Grb2: Optimization of the X+1 Position of 3-Amino-Z-Tyr(PO3H2)-X+1-Asn-NH2

Entry into a new class of protein kinase inhibitors by pseudo ring design

Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors

Structural basis for specificity of GRB2-SH2 revealed by a novel ligand binding mode

Protein kinases as targets for anticancer agents: from inhibitors to useful drugs

Epothilones and Their Analogs – Potential New Weapons in the Fight Against Cancer

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors

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