Literature DB >> 17826092

Optimization of triarylimidazoles for Tie2: influence of conformation on potency.

Neil W Johnson1, Marcus Semones, Jerry L Adams, Michael Hansbury, Jim Winkler.   

Abstract

In an effort to understand the effect of N-alkylation of triarylimidazoles on Tie2 inhibition, ortho-substituted C-2 aryl analogs were synthesized to investigate the effect of different torsion angles on potency. This exercise resulted in the identification of a potent and selective tetrasubstituted imidazole that was efficacious in an animal model of angiogenesis.

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Year:  2007        PMID: 17826092     DOI: 10.1016/j.bmcl.2007.08.052

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


  2 in total

1.  A palladium-catalyzed synthesis of (hetero)aryl-substituted imidazoles from aryl halides, imines and carbon monoxide.

Authors:  Jevgenijs Tjutrins; Bruce A Arndtsen
Journal:  Chem Sci       Date:  2016-11-03       Impact factor: 9.825

2.  Modular Synthesis of Di- and Trisubstituted Imidazoles from Ketones and Aldehydes: A Route to Kinase Inhibitors.

Authors:  Ian de Toledo; Thiago A Grigolo; James M Bennett; Jonathan M Elkins; Ronaldo A Pilli
Journal:  J Org Chem       Date:  2019-09-30       Impact factor: 4.354

  2 in total

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