Literature DB >> 19665377

Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.

Zakaria Rachid1, Meaghan Macphee, Christopher Williams, Margarita Todorova, Bertrand Jacques Jean-Claude.   

Abstract

The monoalkyltriazene moiety lends itself well to the design of combi-molecules. However, due to its instability under physiological conditions, efforts were directed towards stabilizing it by grafting a hydrolysable carbamate onto the 3-position. The synthesis and biological activities of these novel N-carbamyl triazenes are described.

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Year:  2009        PMID: 19665377     DOI: 10.1016/j.bmcl.2009.05.060

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


  4 in total

1.  ZRX1, the first EGFR inhibitor-capecitabine based combi-molecule, requires carboxylesterase-mediated hydrolysis for optimal activity.

Authors:  Maria Ait-Tihyaty; Zakaria Rachid; Anne-Laure Larroque-Lombard; Bertrand J Jean-Claude
Journal:  Invest New Drugs       Date:  2013-12       Impact factor: 3.850

2.  Characterization of the potency of epidermal growth factor (EGFR)-DNA targeting combi-molecules containing a hydrolabile carbamate at the 3-position of the triazene chain.

Authors:  Meaghan MacPhee; Zakaria Rachid; Margarita Todorova; Qiyu Qiu; Gina Belinsky; Bertrand J Jean-Claude
Journal:  Invest New Drugs       Date:  2010-04-29       Impact factor: 3.850

Review 3.  Chemical characteristics, synthetic methods, and biological potential of quinazoline and quinazolinone derivatives.

Authors:  Mohammad Asif
Journal:  Int J Med Chem       Date:  2014-11-12

4.  Subcellular distribution and mechanism of action of AL906, a novel and potent EGFR inhibitor rationally designed to be green fluorescent.

Authors:  Nahid Golabi; Anne-Laure Larroque; Lisa Peyrard; Christopher Williams; Bertrand J Jean-Claude
Journal:  Invest New Drugs       Date:  2020-07-09       Impact factor: 3.850

  4 in total

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