Literature DB >> 16055332

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.

Peter Ballard1, Robert H Bradbury, Laurent F A Hennequin, D Mark Hickinson, Paul D Johnson, Jason G Kettle, Teresa Klinowska, Remy Morgentin, Donald J Ogilvie, Annie Olivier.   

Abstract

Starting from a 6,7-substituted quinazoline lead 4, optimisation of 5-substituted quinazolines containing an extended aniline motif led to potent and selective inhibitors of erbB2 receptor tyrosine kinase, and a representative compound 12a inhibited tumour growth in a mouse xenograft model.

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Year:  2005        PMID: 16055332     DOI: 10.1016/j.bmcl.2005.06.068

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


  3 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

2.  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

3.  Src and ADAM-17-mediated shedding of transforming growth factor-alpha is a mechanism of acute resistance to TRAIL.

Authors:  Sandra Van Schaeybroeck; Donal M Kelly; Joan Kyula; Susan Stokesberry; Dean A Fennell; Patrick G Johnston; Daniel B Longley
Journal:  Cancer Res       Date:  2008-10-15       Impact factor: 12.701

  3 in total

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