Literature DB >> 15727879

Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase.

Søren Ebdrup1, Poul Jacobsen, Anupma Dhanda Farrington, Per Vedsø.   

Abstract

A range of aryl and heteroaryl boronic acids were tested for their in vitro hormone-sensitive lipase inhibitory properties. (2-Benzyloxy-5-fluorophenyl)boronic acid, (2-benzyloxy-5-chlorophenyl)boronic acid and 5-bromothiophene-2-boronic acid were found to be the most potent HSL inhibitors with IC(50) values of 140, 17 and 350 nM, respectively.

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Year:  2005        PMID: 15727879     DOI: 10.1016/j.bmc.2004.12.042

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  Iterative Cross-Couplng with MIDA Boronates: Towards a General Platform for Small Molecule Synthesis.

Authors:  Eric P Gillis; Martin D Burke
Journal:  Aldrichimica Acta       Date:  2009       Impact factor: 3.667

2.  Rat hormone sensitive lipase inhibition by cyclipostins and their analogs.

Authors:  Elena Vasilieva; Supratik Dutta; Raj K Malla; Benjamin P Martin; Christopher D Spilling; Cynthia M Dupureur
Journal:  Bioorg Med Chem       Date:  2015-01-22       Impact factor: 3.641

3.  Water-soluble BODIPY-nido-carborane nanoparticles applied to biocompatibility tumor cell imaging.

Authors:  Dongfang Dai; Guangchang Lian; Xia He; Jifeng Feng; Guofan Jin
Journal:  Photochem Photobiol Sci       Date:  2022-01-21       Impact factor: 3.982

4.  The lipidome and proteome of oil bodies from Helianthus annuus (common sunflower).

Authors:  Samuel Furse; Susan Liddell; Catharine A Ortori; Huw Williams; D Cameron Neylon; David J Scott; David A Barrett; David A Gray
Journal:  J Chem Biol       Date:  2013-01-26

Review 5.  Boronic Acids and Their Derivatives in Medicinal Chemistry: Synthesis and Biological Applications.

Authors:  Mariana Pereira Silva; Lucília Saraiva; Madalena Pinto; Maria Emília Sousa
Journal:  Molecules       Date:  2020-09-21       Impact factor: 4.411

  5 in total

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