Literature DB >> 17869514

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Peter Ballard1, Bernard C Barlaam, Robert H Bradbury, Allan Dishington, Laurent F A Hennequin, D Mark Hickinson, Ian M Hollingsworth, Jason G Kettle, Teresa Klinowska, Donald J Ogilvie, Stuart E Pearson, James S Scott, Abid Suleman, Robin Whittaker, Emma J Williams, Robin Wood, Lindsay Wright.   

Abstract

Neutral 5-substituted 4-anilinoquinazolines addressed high in vivo clearance and phospholipidosis associated with previous basic compounds. A representative compound 8a inhibited tumor growth in a mouse xenograft model when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT), and data are consistent with pharmacology primarily reflecting inhibition of erbB2 receptor tyrosine kinase.

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Year:  2007        PMID: 17869514     DOI: 10.1016/j.bmcl.2007.08.073

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


  3 in total

1.  Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.

Authors:  Jianwei Wu; Wenteng Chen; Guangxin Xia; Jing Zhang; Jiaan Shao; Biqin Tan; Chunchun Zhang; Wanwan Yu; Qinjie Weng; Haiyan Liu; Miao Hu; Hailin Deng; Yu Hao; Jingkang Shen; Yongping Yu
Journal:  ACS Med Chem Lett       Date:  2013-08-06       Impact factor: 4.345

2.  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

3.  1-Aminobenzotriazole: A Mechanism-Based Cytochrome P450 Inhibitor and Probe of Cytochrome P450 Biology.

Authors:  Paul R Ortiz de Montellano
Journal:  Med Chem (Los Angeles)       Date:  2018-03-31
  3 in total

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