Literature DB >> 14741286

Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.

Thierry Le Diguarher1, Jean-Claude Ortuno, David Shanks, Nicolas Guilbaud, Alain Pierré, Eric Raimbaud, Jean-Luc Fauchère, John A Hickman, Gordon C Tucker, Patrick J Casara.   

Abstract

A structure-activity study was performed by synthesis on N,N'-disubstitution of 3-aminobenzo[c] and [d]azepin-2-one 2 and 3 to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities.

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Year:  2004        PMID： 14741286     DOI： 10.1016/j.bmcl.2003.11.013

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


  3 in total

1.  Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.

Authors:  Olivier Van der Poorten; Krisztina Fehér; Koen Buysse; Debby Feytens; Ioanna Zoi; Steven D Schwartz; José C Martins; Dirk Tourwé; Minying Cai; Victor J Hruby; Steven Ballet
Journal:  ACS Med Chem Lett       Date:  2014-12-03       Impact factor: 4.345

2.  Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.

Authors:  Steven Ballet; Alexander V Mayorov; Minying Cai; Dagmara Tymecka; Kevin B Chandler; Erin S Palmer; Karolien Van Rompaey; Aleksandra Misicka; Dirk Tourwé; Victor J Hruby
Journal:  Bioorg Med Chem Lett       Date:  2007-02-09       Impact factor: 2.823

3.  Phosphine-Catalyzed α-Umpolung-Aldol Reaction for the Synthesis of Benzo[ b]azapin-3-ones.

Authors:  Kui Zhang; Lingchao Cai; Sooji Hong; Ohyun Kwon
Journal:  Org Lett       Date:  2019-06-20       Impact factor: 6.005
  3 in total

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