Literature DB >> 16427279

Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold.

Walfrido Antuch1, Sanjay Menon, Quin-Zene Chen, Yingchun Lu, Sukumar Sakamuri, Barbara Beck, Vesna Schauer-Vukasinović, Seema Agarwal, Sibylle Hess, Alexander Dömling.   

Abstract

A terphenyl alpha-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.

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Year:  2006        PMID: 16427279     DOI: 10.1016/j.bmcl.2005.11.102

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


  12 in total

1.  Heterocyclic alpha-helix mimetics for targeting protein-protein interactions.

Authors:  Shannon M Biros; Lionel Moisan; Enrique Mann; Alexandre Carella; Dayong Zhai; John C Reed; Julius Rebek
Journal:  Bioorg Med Chem Lett       Date:  2007-05-27       Impact factor: 2.823

2.  Multicomponent synthesis of dihydrobenzoxazepinones, bearing four diversity points, as potential α-helix mimics.

Authors:  Luca Banfi; Andrea Basso; Valentina Cerulli; Giuseppe Guanti; Paulina Lecinska; Ilaria Monfardini; Renata Riva
Journal:  Mol Divers       Date:  2009-11-28       Impact factor: 2.943

Review 3.  Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.

Authors:  Duncan E Scott; Andrew R Bayly; Chris Abell; John Skidmore
Journal:  Nat Rev Drug Discov       Date:  2016-04-11       Impact factor: 84.694

4.  1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Chem Biol Drug Des       Date:  2010-06-09       Impact factor: 2.817

5.  Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.

Authors:  Landon R Whitby; Yoshio Ando; Vincent Setola; Peter K Vogt; Bryan L Roth; Dale L Boger
Journal:  J Am Chem Soc       Date:  2011-06-15       Impact factor: 15.419

6.  Cyanoacetamide MCR (III): three-component Gewald reactions revisited.

Authors:  Kan Wang; Dabin Kim; Alexander Dömling
Journal:  J Comb Chem       Date:  2010 Jan-Feb

7.  The p53-MDM2/MDMX axis - A chemotype perspective.

Authors:  Kareem Khoury; Grzegorz M Popowicz; Tad A Holak; Alexander Dömling
Journal:  Medchemcomm       Date:  2011       Impact factor: 3.597

8.  A Van Leusen deprotection-cyclization strategy as a fast entry into two imidazoquinoxaline families.

Authors:  Fabio De Moliner; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2012-08-24       Impact factor: 2.415

9.  Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions.

Authors:  Alex Shaginian; Landon R Whitby; Sukwon Hong; Inkyu Hwang; Bilal Farooqi; Mark Searcey; Jiandong Chen; Peter K Vogt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2009-04-22       Impact factor: 15.419

10.  Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.

Authors:  Jacob J Kalbfleisch; Carson W Reed; Charlotte Park; Paul K Spearing; Marc C Quitalig; Matthew T Jenkins; Alice L Rodriguez; Anna L Blobaum; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2020-09-02       Impact factor: 2.823

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