Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity

Hwei-Ru Tsou; Elsebe G. Overbeek-Klumpers; William A. Hallett; Marvin F. Reich; M. Brawner Floyd; Bernard D. Johnson; Ronald S. Michalak; Ramaswamy Nilakantan; Carolyn Discafani; Jonathan Golas; Sridhar K. Rabindran; Ru Shen; Xiaoqing Shi; Yu-Fen Wang; Janis Upeslacis; Allan Wissner

doi:10.1021/jm040159c

Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity

Journal of Medicinal Chemistry ◽

10.1021/jm040159c ◽

2005 ◽

Vol 48 (4) ◽

pp. 1107-1131 ◽

Cited By ~ 191

Author(s):

Hwei-Ru Tsou ◽

Elsebe G. Overbeek-Klumpers ◽

William A. Hallett ◽

Marvin F. Reich ◽

M. Brawner Floyd ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Kinase Activity ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Irreversible Inhibitors ◽

Epidermal Growth ◽

Orally Active

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Discovery of a Potent, Selective, and Orally Active Human Epidermal Growth Factor Receptor-2 Sheddase Inhibitor for the Treatment of Cancer†

Journal of Medicinal Chemistry ◽

10.1021/jm061344o ◽

2007 ◽

Vol 50 (4) ◽

pp. 603-606 ◽

Cited By ~ 22

Author(s):

Wenqing Yao ◽

Jincong Zhuo ◽

David M. Burns ◽

Meizhong Xu ◽

Colin Zhang ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Epidermal Growth ◽

Orally Active

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6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases with Enhanced Antitumor Activity

Journal of Medicinal Chemistry ◽

10.1021/jm0005555 ◽

2001 ◽

Vol 44 (17) ◽

pp. 2719-2734 ◽

Cited By ~ 189

Author(s):

Hwei-Ru Tsou ◽

Nellie Mamuya ◽

Bernard D. Johnson ◽

Marvin F. Reich ◽

Brian C. Gruber ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Antitumor Activity ◽

Tyrosine Kinases ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Irreversible Inhibitors ◽

Her 2 ◽

Epidermal Growth

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Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)

Journal of Medicinal Chemistry ◽

10.1021/jm020241c ◽

2003 ◽

Vol 46 (1) ◽

pp. 49-63 ◽

Cited By ~ 164

Author(s):

Allan Wissner ◽

Elsebe Overbeek ◽

Marvin F. Reich ◽

M. Brawner Floyd ◽

Bernard D. Johnson ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Kinase Activity ◽

Growth Factor Receptor ◽

Irreversible Inhibitor ◽

Structure Activity ◽

Her 2 ◽

Epidermal Growth ◽

Orally Active

Download Full-text

Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b00883 ◽

2016 ◽

Vol 59 (17) ◽

pp. 8103-8124 ◽

Cited By ~ 24

Author(s):

Jeff B. Smaill ◽

Andrea J. Gonzales ◽

Julie A. Spicer ◽

Helen Lee ◽

Jessica E. Reed ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Kinase Inhibitors ◽

Growth Factor Receptor ◽

Pyrimidine Derivatives ◽

Irreversible Inhibitors ◽

Epidermal Growth ◽

Orally Active ◽

Receptor Family

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Faculty Opinions recommendation of Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1064706.517617 ◽

2007 ◽

Author(s):

Thomas W von Geldern

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Epidermal Growth ◽

Orally Active

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ChemInform Abstract: 6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases with Enhanced Antitumor Activity.

ChemInform ◽

10.1002/chin.200149115 ◽

2010 ◽

Vol 32 (49) ◽

pp. no-no

Author(s):

Hwei-Ru Tsou ◽

et al. et al.

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Antitumor Activity ◽

Tyrosine Kinases ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Irreversible Inhibitors ◽

Her 2 ◽

Epidermal Growth

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Faculty Opinions recommendation of Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1011196.178312 ◽

2003 ◽

Author(s):

Steven Bass

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Kinase Activity ◽

Growth Factor Receptor ◽

Irreversible Inhibitor ◽

Structure Activity ◽

Her 2 ◽

Epidermal Growth ◽

Orally Active

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DETECT V – Nachweis von Östrogenrezeptor und Human Epidermal Growth Factor Receptor 2 mittels CellSearch CXC Kit

Senologie - Zeitschrift für Mammadiagnostik und -therapie ◽

10.1055/s-0036-1583408 ◽

2016 ◽

Vol 13 (02) ◽

Author(s):

F Meier-Stiegen ◽

S Riethdorf ◽

A Schramm ◽

A Polasik ◽

D Niederacher ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Growth Factor Receptor ◽

Human Epidermal Growth Factor ◽

Epidermal Growth

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Detection of Human Epidermal Growth Factor Receptor 2 through ICC and FISH in Formalin-Fixed Breast Carcinoma from Cell Block and Correlation of Results to Corresponding Histological Specimens

10.26226/morressier.57d6b2bdd462b8028d88cd87 ◽

2016 ◽

Author(s):

Divya Verma

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Breast Carcinoma ◽

Epidermal Growth Factor ◽

Growth Factor Receptor ◽

Cell Block ◽

Human Epidermal Growth Factor ◽

Epidermal Growth ◽

Formalin Fixed

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Real World Study of Pyrotinib in Human Epidermal Growth Factor Receptor-2 (HER2) Positive Breast Cancer

Case Medical Research ◽

10.31525/ct1-nct04158505 ◽

2019 ◽

Author(s):

Keyword(s):

Breast Cancer ◽

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Real World ◽

Growth Factor Receptor ◽

Her2 Positive ◽

Human Epidermal Growth Factor ◽

Epidermal Growth ◽

Positive Breast Cancer

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