Literature DB >> 14684309

Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.

Yue-Mei Zhang1, Stuart Cockerill, Stephen B Guntrip, David Rusnak, Kathryn Smith, Dana Vanderwall, Edgar Wood, Karen Lackey.   

Abstract

A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC(50) values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.

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Year:  2004        PMID: 14684309     DOI: 10.1016/j.bmcl.2003.10.010

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


  6 in total

1.  Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.

Authors:  Xiaoqing Wu; Mingdong Li; Yang Qu; Wenhua Tang; Youguang Zheng; Jiqin Lian; Min Ji; Liang Xu
Journal:  Bioorg Med Chem       Date:  2010-04-21       Impact factor: 3.641

2.  Design, synthesis, and in vitro antitumor activity evaluation of novel 4-pyrrylamino quinazoline derivatives.

Authors:  Xiaoqing Wu; Mingdong Li; Wenhua Tang; Youguang Zheng; Jiqin Lian; Liang Xu; Min Ji
Journal:  Chem Biol Drug Des       Date:  2011-10-24       Impact factor: 2.817

3.  On the Integration of In Silico Drug Design Methods for Drug Repurposing.

Authors:  Eric March-Vila; Luca Pinzi; Noé Sturm; Annachiara Tinivella; Ola Engkvist; Hongming Chen; Giulio Rastelli
Journal:  Front Pharmacol       Date:  2017-05-23       Impact factor: 5.810

Review 4.  The Development of CK2 Inhibitors: From Traditional Pharmacology to in Silico Rational Drug Design.

Authors:  Giorgio Cozza
Journal:  Pharmaceuticals (Basel)       Date:  2017-02-20

5.  An Integrated System Biology Approach Yields Drug Repositioning Candidates for the Treatment of Heart Failure.

Authors:  Guodong Yang; Aiqun Ma; Zhaohui S Qin
Journal:  Front Genet       Date:  2019-09-25       Impact factor: 4.599

6.  Crystal structure of N-(2-benzoyl-5-ethynylphen-yl)quinoline-2-carboxamide.

Authors:  Diana Peña-Solórzano; Burkhard König; Cesar A Sierra; Cristian Ochoa-Puentes
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2017-03-28
  6 in total

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