Literature DB >> 16516473

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Laurent F A Hennequin1, Peter Ballard, F Tom Boyle, Bénédicte Delouvrié, Rebecca P A Ellston, Chris T Halsall, Craig S Harris, Kevin Hudson, Jane Kendrew, J Elizabeth Pease, Helen S Ross, Peter Smith, Jennifer L Vincent.   

Abstract

The structure-activity relationship of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains has been investigated. This exploration has led to the discovery of novel aminomethyl carboxamides with good biological, pharmacokinetic and physical properties.

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Year:  2006        PMID： 16516473     DOI： 10.1016/j.bmcl.2006.02.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.

Authors:  Bernard Barlaam; Judith Anderton; Peter Ballard; Robert H Bradbury; Laurent F A Hennequin; D Mark Hickinson; Jason G Kettle; George Kirk; Teresa Klinowska; Christine Lambert-van der Brempt; Cath Trigwell; John Vincent; Donald Ogilvie
Journal:  ACS Med Chem Lett       Date:  2013-05-31       Impact factor: 4.345

Review 2.  Drug repositioning approaches for the discovery of new therapeutics for Alzheimer's disease.

Authors:  Tae-Wan Kim
Journal:  Neurotherapeutics       Date:  2015-01       Impact factor: 7.620

3.  Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer.

Authors:  Peter S Hammerman; Martin L Sos; Alex H Ramos; Chunxiao Xu; Amit Dutt; Wenjun Zhou; Lear E Brace; Brittany A Woods; Wenchu Lin; Jianming Zhang; Xianming Deng; Sang Min Lim; Stefanie Heynck; Martin Peifer; Jeffrey R Simard; Michael S Lawrence; Robert C Onofrio; Helga B Salvesen; Danila Seidel; Thomas Zander; Johannes M Heuckmann; Alex Soltermann; Holger Moch; Mirjam Koker; Frauke Leenders; Franziska Gabler; Silvia Querings; Sascha Ansén; Elisabeth Brambilla; Christian Brambilla; Philippe Lorimier; Odd Terje Brustugun; Aslaug Helland; Iver Petersen; Joachim H Clement; Harry Groen; Wim Timens; Hannie Sietsma; Erich Stoelben; Jürgen Wolf; David G Beer; Ming Sound Tsao; Megan Hanna; Charles Hatton; Michael J Eck; Pasi A Janne; Bruce E Johnson; Wendy Winckler; Heidi Greulich; Adam J Bass; Jeonghee Cho; Daniel Rauh; Nathanael S Gray; Kwok-Kin Wong; Eric B Haura; Roman K Thomas; Matthew Meyerson
Journal:  Cancer Discov       Date:  2011-06       Impact factor: 39.397

4.  3D-QSAR and molecular docking studies of 4-anilinoquinazoline derivatives: a rational approach to anticancer drug design.

Authors:  Sisir Nandi; Manish C Bagchi
Journal:  Mol Divers       Date:  2009-03-28       Impact factor: 2.943

5.  Development and application of high-throughput screens for the discovery of compounds that disrupt ErbB4 signaling: Candidate cancer therapeutics.

Authors:  Richard L Cullum; Lauren M Lucas; Jared I Senfeld; John T Piazza; Logan T Neel; Kanupriya Whig; Ling Zhai; Mackenzie H Harris; Cristina C Rael; Darby C Taylor; Laura J Cook; David P Kaufmann; Christopher P Mill; Megan A Jacobi; Forrest T Smith; Mark Suto; Robert Bostwick; Ram B Gupta; Allan E David; David J Riese Ii
Journal:  PLoS One       Date:  2020-12-30       Impact factor: 3.240
  5 in total

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