Terry V. Hughes

Correction to Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel

Pamela A. Haile, Linda Casillas, Michael J. Bury, John F. Mehlmann et autres

[This corrects the article DOI: 10.1021/acsmedchemlett.8b00344.].

Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors

Curt D. Haffner, Adam K. Charnley, Christopher Aquino, Linda Casillas et autres

Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2). Fragment based screening and design principles led to the identification of the inhibitor series, and X-ray crystallography was used to inform …

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Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel

Pamela A. Haile, Linda Casillas, Michael J. Bury, John F. Mehlmann et autres

RIP2 kinase was recently identified as a therapeutic target for a variety of autoimmune diseases. We have reported previously a selective 4-aminoquinoline-based RIP2 inhibitor GSK583 and demonstrated its effectiveness in blocking downstream NOD2 signaling in cellular models, rodent in vivo models, and …

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Author response: Donated chemical probes for open science

Susanne Müller, Suzanne Ackloo, C.H. Arrowsmith, Marcus Bauser et autres

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Abstract 2456: Discovery of orally active 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes with dual EGFR and HER2 inhibitory activity.

Peter J. Connolly, Mary Adams, Amanda K. Beck, Stuart L. Emanuel et autres

Abstract Growth factor receptors of the ErbB family, especially ErbB1 (EGFR) and ErbB2 (HER2), have attracted considerable attention in recent years as therapeutic targets for the treatment of numerous malignancies including cancers of the lung, colon, and breast, either through blockade of …

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N-Chlorosuccinimide

Scott C. Virgil, Terry V. Hughes, Di Qiu, Jianbo Wang

[128-09-6] C4H4ClNO2 (MW 133.53) InChI = 1S/C4H4ClNO2/c5-6-3(7)1-2-4(6)8/h1-2H2 InChIKey = JRNVZBWKYDBUCA-UHFFFAOYSA-N (electrophilic α-chlorination of sulfides, sulfoxides, and ketones; preparation of N-chloroamines) Alternative Names: 1-chloro-2,5-pyrrolidinedione; NCS. Physical Data: mp 144–146 °C. Solubility: sol H2O; sl sol CCl4, benzene, toluene, AcOH; insol ether. Form Supplied …

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President's Report 2010-2011

J.A. Carlson, Rita Gubbels, Mary Therese Gubbles, Patricia Gildersleeve et autres

Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Ronghui Lin, Sigmond G. Johnson, Peter J. Connolly, Steven K. Wetter et autres

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7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity

Terry V. Hughes, Stuart L. Emanuel, Harold R. O’Grady, Peter J. Connolly et autres

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A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: Design, synthesis, and biological activity

Terry V. Hughes, Guozhang Xu, Steven K. Wetter, Peter J. Connolly et autres

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Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases

Guozhang Xu, Lily L. Searle, Terry V. Hughes, Amanda K. Beck et autres

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Cellular and in Vivo Activity of JNJ-28871063, A Nonquinazoline Pan-ErbB Kinase Inhibitor That Crosses the Blood-Brain Barrier and Displays Efficacy against Intracranial Tumors

Stuart L. Emanuel, Terry V. Hughes, Mary Adams, Catherine A. Rugg et autres

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