Literature DB >> 9873717

Novel phosphate mimetics for the design of non-peptidyl inhibitors of protein tyrosine phosphatases.

C C Kotoris1, M J Chen, S D Taylor.   

Abstract

Benzylic alpha,alpha-difluorosulfonates, alpha,alpha-difluorotetrazoles, and alpha,alpha-difluorocarboxylates of type 5 and 6 were synthesized and examined as potential phosphate biosteres for PTP1B inhibition. The alpha,alpha-difluorosulfonates and alpha,alpha-difluorotetrazoles were found to be more effective inhibitors than the analogous compounds bearing the fluoromalonyl group, a phosphate biostere currently being used for PTP inhibition.

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Year:  1998        PMID: 9873717     DOI: 10.1016/s0960-894x(98)00598-8

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


  5 in total

1.  Structure-based prediction of free energy changes of binding of PTP1B inhibitors.

Authors:  Jing Wang; Shek Ling Chan; Kal Ramnarayan
Journal:  J Comput Aided Mol Des       Date:  2003-08       Impact factor: 3.686

2.  Design and synthesis of nonpeptidic, small molecule inhibitors for the Mycobacterium tuberculosis protein tyrosine phosphatase PtpB.

Authors:  Katherine A Rawls; Christoph Grundner; Jonathan A Ellman
Journal:  Org Biomol Chem       Date:  2010-07-19       Impact factor: 3.876

3.  A two stage click-based library of protein tyrosine phosphatase inhibitors.

Authors:  Jian Xie; Christopher T Seto
Journal:  Bioorg Med Chem       Date:  2006-10-12       Impact factor: 3.641

4.  Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases.

Authors:  Lok Hang Mak; Jessica Knott; Katherine A Scott; Claire Scott; Gillian F Whyte; Yu Ye; David J Mann; Oscar Ces; James Stivers; Rudiger Woscholski
Journal:  Bioorg Med Chem       Date:  2012-05-24       Impact factor: 3.641

5.  Effects on polo-like kinase 1 polo-box domain binding affinities of peptides incurred by structural variation at the phosphoamino acid position.

Authors:  Wenjian Qian; Jung-Eun Park; Fa Liu; Kyung S Lee; Terrence R Burke
Journal:  Bioorg Med Chem       Date:  2012-05-26       Impact factor: 3.641

  5 in total

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