Literature DB >> 12951126

Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).

Bin Ye1, Shawn Bauer, Brad O Buckman, Ameen Ghannam, Brian D Griedel, Seock-Kyu Khim, Wheeseong Lee, Karna L Sacchi, Kenneth J Shaw, Amy Liang, Qingyu Wu, Zuchun Zhao.   

Abstract

Compound 1 was identified by high throughput screening as a novel PAI-1 inhibitor. Optimization of the B and C-segments of 1 resulted in a series of structurally simplified compounds with improved potency. The synthesis and SAR data of these compounds are presented here.

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Year:  2003        PMID： 12951126     DOI： 10.1016/s0960-894x(03)00686-3

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


  2 in total

1.  Dual-reporter high-throughput screen for small-molecule in vivo inhibitors of plasminogen activator inhibitor type-1 yields a clinical lead candidate.

Authors:  Ashley A Reinke; Shih-Hon Li; Mark Warnock; Maxim E Shaydakov; Naga Sandhya Guntaka; Enming J Su; Jose A Diaz; Cory D Emal; Daniel A Lawrence
Journal:  J Biol Chem       Date:  2018-12-03       Impact factor: 5.157

2.  Discovery of novel urokinase plasminogen activator (uPA) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.

Authors:  Mahmoud A Al-Sha'er; Mohammad A Khanfar; Mutasem O Taha
Journal:  J Mol Model       Date:  2014-01-28       Impact factor: 1.810
  2 in total

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