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Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)

Journal of medicinal chemistry, 2018-06, Vol.61 (11), p.4704-4719

2018

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Targeting Src and Tubulin in Mucinous Ovarian Carcinoma

Clinical cancer research, 2013-12, Vol.19 (23), p.6532-6543

2013

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Thermodynamic Inhibition Profile of a Cyclopentyl and a Cyclohexyl Derivative towards Thrombin: The Same but for Different Reasons

Angewandte Chemie (International ed.), 2007-01, Vol.46 (44), p.8511-8514

2007

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Enhancement of Hydrophobic Interactions and Hydrogen Bond Strength by Cooperativity: Synthesis, Modeling, and Molecular Dynamics Simulations of a Congeneric Series of Thrombin Inhibitors

Journal of medicinal chemistry, 2010-03, Vol.53 (5), p.2126-2135

2010

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A phase Ib dose escalation study of oral monotherapy with KX2-391 in elderly patients with acute myeloid leukemia

Investigational new drugs, 2022-08, Vol.40 (4), p.773-781

2022

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Binding cooperativity between a ligand carbonyl group and a hydrophobic side chain can be enhanced by additional H-bonds in a distance dependent manner: A case study with thrombin inhibitors

European journal of medicinal chemistry, 2015-05, Vol.96, p.405-424

2015

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Ligand binding cooperativity: Bioisosteric replacement of CO with SO2 among thrombin inhibitors

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (16), p.3850-3854

2016

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Thiazolyl N-benzyl-substituted acetamide derivatives: Synthesis, Src kinase inhibitory and anticancer activities

European journal of medicinal chemistry, 2011-10, Vol.46 (10), p.4853-4858

2011

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KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma

Journal of neuro-oncology, 2018-12, Vol.140 (3), p.519-527

2018

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A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer

Cancer chemotherapy and pharmacology, 2013-04, Vol.71 (4), p.883-892

2013

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A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies

Investigational new drugs, 2013-08, Vol.31 (4), p.967-973

2013

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Ligand binding cooperativity: Bioisosteric replacement of C==O with SO sub(2) among thrombin inhibitors

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (16), p.3850-3854

2016

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An interactive computer graphics study of thermolysin-catalyzed peptide cleavage and inhibition by N-carboxymethyl dipeptides

Biochemistry (Easton), 1984-11, Vol.23 (24), p.5730-5741

1984

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Privileged scaffolds for blocking protein–protein interactions: 1,4-disubstituted naphthalene antagonists of transcription factor complex HOX–PBX/DNA

Bioorganic & medicinal chemistry letters, 2004-08, Vol.14 (15), p.3875-3879

2004

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Application of mechanism-based PKPD model to identify optimal dosing regimens for future development of oraxol

Journal of clinical oncology, 2013, Vol.31 (15_suppl), p.e13505-e13505

2013

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Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells

Biochemistry (Easton), 1989-06, Vol.28 (13), p.5694-5701

1989

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The design, synthesis and activity of non-ATP competitive inhibitors of pp60c-src tyrosine kinase.Part 1: Hydroxynaphthalene derivatives

Bioorganic & medicinal chemistry letters, 2000-03, Vol.10 (5), p.477-481

2000

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Synthesis of a Vicinal Tricarbonyl Amide Derivative of l-Phenylalanine

Journal of organic chemistry, 1996-03, Vol.61 (5), p.1872-1874

1996

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A phase II study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer (CRPC): A PCCTC trial

Journal of clinical oncology, 2012-05, Vol.30 (15_suppl), p.4654-4654

2012

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Abstract 5598: KX02, a novel therapeutic for glioma

Cancer research (Chicago, Ill.), 2010-04, Vol.70 (8_Supplement), p.5598-5598

2010

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Total synthesis of pseudoguaianolides: (.+-.)-aromaticin and (.+-.)-aromatin

Journal of the American Chemical Society, 1980-05, Vol.102 (11), p.3964-3965

1980

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Thermodynamisches Inhibitionsprofil eines Cyclopentyl- und eines Cyclohexylderivats gegenüber Thrombin: gleich, jedoch aus unterschiedlichem Grund

Angewandte Chemie, 2007-11, Vol.119 (44), p.8664-8667

2007

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Identification of efficient pentapeptide substrates for the tyrosine kinase pp60c-src

Journal of medicinal chemistry, 1995-10, Vol.38 (21), p.4276-4283

1995

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Total synthesis of erbstatin

Tetrahedron letters, 1986, Vol.27 (48), p.5799-5802

Hangauer, David G

1986

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The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives

Bioorganic & medicinal chemistry letters, 2000-03, Vol.10 (5), p.483-486

2000

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Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)

Targeting Src and Tubulin in Mucinous Ovarian Carcinoma

Thermodynamic Inhibition Profile of a Cyclopentyl and a Cyclohexyl Derivative towards Thrombin: The Same but for Different Reasons

Enhancement of Hydrophobic Interactions and Hydrogen Bond Strength by Cooperativity: Synthesis, Modeling, and Molecular Dynamics Simulations of a Congeneric Series of Thrombin Inhibitors

A phase Ib dose escalation study of oral monotherapy with KX2-391 in elderly patients with acute myeloid leukemia

Binding cooperativity between a ligand carbonyl group and a hydrophobic side chain can be enhanced by additional H-bonds in a distance dependent manner: A case study with thrombin inhibitors

Ligand binding cooperativity: Bioisosteric replacement of CO with SO2 among thrombin inhibitors

Thiazolyl N-benzyl-substituted acetamide derivatives: Synthesis, Src kinase inhibitory and anticancer activities

KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma

A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer

A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies

Ligand binding cooperativity: Bioisosteric replacement of C==O with SO sub(2) among thrombin inhibitors

An interactive computer graphics study of thermolysin-catalyzed peptide cleavage and inhibition by N-carboxymethyl dipeptides

Privileged scaffolds for blocking protein–protein interactions: 1,4-disubstituted naphthalene antagonists of transcription factor complex HOX–PBX/DNA

Application of mechanism-based PKPD model to identify optimal dosing regimens for future development of oraxol

Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells

The design, synthesis and activity of non-ATP competitive inhibitors of pp60c-src tyrosine kinase.Part 1: Hydroxynaphthalene derivatives

Synthesis of a Vicinal Tricarbonyl Amide Derivative of l-Phenylalanine

A phase II study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer (CRPC): A PCCTC trial

Abstract 5598: KX02, a novel therapeutic for glioma

Total synthesis of pseudoguaianolides: (.+-.)-aromaticin and (.+-.)-aromatin

Thermodynamisches Inhibitionsprofil eines Cyclopentyl- und eines Cyclohexylderivats gegenüber Thrombin: gleich, jedoch aus unterschiedlichem Grund

Identification of efficient pentapeptide substrates for the tyrosine kinase pp60c-src

Total synthesis of erbstatin

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives

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