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Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer

Proceedings of the National Academy of Sciences - PNAS, 2017-03, Vol.114 (12), p.3127-3132

2017

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Functional Characterization of CFI-400945, a Polo-like Kinase 4 Inhibitor, as a Potential Anticancer Agent

Cancer cell, 2014-08, Vol.26 (2), p.163-176

2014

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The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3‑(4-(heterocyclyl)phenyl)‑1H‑indazole-5-carboxamides as Anticancer Agents

Journal of medicinal chemistry, 2015-04, Vol.58 (8), p.3366-3392

2015

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Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides

Bioorganic & medicinal chemistry, 2014-09, Vol.22 (17), p.4968-4997

2014

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An evolved ribosome-inactivating protein targets and kills human melanoma cells in vitro and in vivo

Molecular cancer, 2010-02, Vol.9 (1), p.28-28, Article 28

2010

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(111)In-labeled EGF is selectively radiotoxic to human breast cancer cells overexpressing EGFR

The Journal of nuclear medicine (1978), 2000-03, Vol.41 (3), p.429

2000

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The Discovery of Polo-Like Kinase 4 Inhibitors: Design and Optimization of Spiro[cyclopropane-1,3′[3H]indol]-2′(1′H)‑ones as Orally Bioavailable Antitumor Agents

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.130-146

2015

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Abstract PD2-03: CDK4/6 inhibitor-resistant ER+ breast cancer cell lines are hypersensitive to TTK inhibition

Cancer research (Chicago, Ill.), 2020-02, Vol.80 (4_Supplement), p.PD2-03-PD2-03

2020

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Abstract 1642: Evaluation of ENMD-2076 in combination with anti-PD1 in syngeneic cancer models

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.1642-1642

2017

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The Discovery of PLK4 Inhibitors: (E)‑3-((1H‑Indazol-6-yl)methylene)indolin-2-ones as Novel Antiproliferative Agents

Journal of medicinal chemistry, 2013-08, Vol.56 (15), p.6069-6087

2013

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Discovery of Pyrazolo[1,5‑a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent

ACS medicinal chemistry letters, 2016-07, Vol.7 (7), p.671-675

2016

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The spindle assembly checkpoint is a therapeutic vulnerability of CDK4/6 inhibitor–resistant ER + breast cancer with mitotic aberrations

Science advances, 2022-09, Vol.8 (36), p.eabq4293-eabq4293

2022

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Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3′-indolin]-2′-ones as potent PLK4 inhibitors with oral antitumor efficacy

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (19), p.4625-4630

2016

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Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (15), p.3562-3566

2016

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The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.130-146

2015

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Abstract B267: Inhibition of PLK4 as a therapeutic strategy for genomically unstable cancers deficient for PTEN

Molecular cancer therapeutics, 2013-11, Vol.12 (11_Supplement), p.B267-B267

2013

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The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1 H -indazole-5-carboxamides as Anticancer Agents

Journal of medicinal chemistry, 2015-04, Vol.58 (8), p.3366-3392

2015

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Abstract 4507: Discovery of a novel single chain ribosome inactivating protein that selectively kills human melanoma cells

Cancer research (Chicago, Ill.), 2010-04, Vol.70 (8_Supplement), p.4507-4507

2010

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Abstract LB-215: Inhibition of Polo-like kinase 4 as an anti-cancer strategy

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.LB-215-LB-215

2011

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Penetration and Intracellular Routing of Nucleus-Directed Peptide-Based Shuttles (Loligomers) in Eukaryotic Cells

Biochemistry (Easton), 1998-04, Vol.37 (17), p.5798-5809

1998

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A comparsion of EGF and MAb 528 labeled with (111)In for imaging human breast cancer

The Journal of nuclear medicine (1978), 2000-05, Vol.41 (5), p.903

2000

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Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer

Functional Characterization of CFI-400945, a Polo-like Kinase 4 Inhibitor, as a Potential Anticancer Agent

Carnitine palmitoyltransferase 1C promotes cell survival and tumor growth under conditions of metabolic stress

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3‑(4-(heterocyclyl)phenyl)‑1H‑indazole-5-carboxamides as Anticancer Agents

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides

An evolved ribosome-inactivating protein targets and kills human melanoma cells in vitro and in vivo

(111)In-labeled EGF is selectively radiotoxic to human breast cancer cells overexpressing EGFR

The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1R,2S)‑2-(3-((E)‑4-(((cis)‑2,6-Dimethylmorpholino)methyl)styryl)‑1H‑indazol-6-yl)-5′-methoxyspiro[cyclopropane-1,3′-indolin]-2′-one (CFI-400945) as a Potent, Orally Active Antitumor Agent

The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1 R ,2 S )-2-(3-(( E )-4-((( cis )-2,6-Dimethylmorpholino)methyl)styryl)-1 H -indazol-6-yl)-5′-methoxyspiro[cyclopropane-1,3′-indolin]-2′-one (CFI-400945) as a Potent, Orally Active Antitumor Agent

The Discovery of Polo-Like Kinase 4 Inhibitors: Design and Optimization of Spiro[cyclopropane-1,3′[3H]indol]-2′(1′H)‑ones as Orally Bioavailable Antitumor Agents

Abstract PD2-03: CDK4/6 inhibitor-resistant ER+ breast cancer cell lines are hypersensitive to TTK inhibition

Abstract 1642: Evaluation of ENMD-2076 in combination with anti-PD1 in syngeneic cancer models

The Discovery of PLK4 Inhibitors: (E)‑3-((1H‑Indazol-6-yl)methylene)indolin-2-ones as Novel Antiproliferative Agents

Discovery of Pyrazolo[1,5‑a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent

The spindle assembly checkpoint is a therapeutic vulnerability of CDK4/6 inhibitor–resistant ER + breast cancer with mitotic aberrations

Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3′-indolin]-2′-ones as potent PLK4 inhibitors with oral antitumor efficacy

Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK

The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents

Abstract B267: Inhibition of PLK4 as a therapeutic strategy for genomically unstable cancers deficient for PTEN

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1 H -indazole-5-carboxamides as Anticancer Agents

Abstract 4507: Discovery of a novel single chain ribosome inactivating protein that selectively kills human melanoma cells

Abstract LB-215: Inhibition of Polo-like kinase 4 as an anti-cancer strategy

The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent

Penetration and Intracellular Routing of Nucleus-Directed Peptide-Based Shuttles (Loligomers) in Eukaryotic Cells

A comparsion of EGF and MAb 528 labeled with (111)In for imaging human breast cancer

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