Literature DB >> 14611852

Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.

Kevin R Guertin1, Lina Setti, Lida Qi, Rachel M Dunsdon, Brian W Dymock, Philip S Jones, Hilary Overton, Mathew Taylor, Glyn Williams, Joseph A Sergi, Karen Wang, Ying Peng, Marcia Renzetti, Rogely Boyce, Fiorenza Falcioni, Ralph Garippa, Andrée R Olivier.   

Abstract

A novel series of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents have been identified. These compounds show non-selective inhibitory properties against a panel of protein tyrosine phosphatases including PTP1B. Compounds 12 and 13 display oral glucose lowering effects in ob/ob mice.

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Year:  2003        PMID： 14611852     DOI： 10.1016/s0960-894x(03)00623-1

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


  8 in total

Review 1.  Small molecule tools for functional interrogation of protein tyrosine phosphatases.

Authors:  Rongjun He; Li-Fan Zeng; Yantao He; Sheng Zhang; Zhong-Yin Zhang
Journal:  FEBS J       Date:  2012-08-16       Impact factor: 5.542

2.  Discovery of the First Non-cGMP Mimetic Small Molecule Activators of cGMP-Dependent Protein Kinase 1 α (PKG1α).

Authors:  Jennifer Hanisak; Aileen Soriano; Gregory C Adam; Andrea Basso; David Bauman; David Bell; Emily Frank; Gregory O'Donnell; Paul Tawa; Andreas Verras; Yang Yu; Lei Zhang; W Michael Seganish
Journal:  ACS Med Chem Lett       Date:  2021-07-16       Impact factor: 4.632

3.  High throughput screening for small molecule inhibitors of heparin-induced tau fibril formation.

Authors:  Alex Crowe; Carlo Ballatore; Edward Hyde; John Q Trojanowski; Virginia M-Y Lee
Journal:  Biochem Biophys Res Commun       Date:  2007-03-19       Impact factor: 3.575

4.  Isoquinoline-1,3,4-trione derivatives inactivate caspase-3 by generation of reactive oxygen species.

Authors:  Jun-Qing Du; Jian Wu; Hua-Jie Zhang; Ya-Hui Zhang; Bei-Ying Qiu; Fang Wu; Yi-Hua Chen; Jing-Ya Li; Fa-Jun Nan; Jian-Ping Ding; Jia Li
Journal:  J Biol Chem       Date:  2008-09-02       Impact factor: 5.157

5.  Synthesis, molecular structure and characterization of allylic derivatives of 6-amino-3-methyl-1,2,4-triazolo[3,4-f][1,2,4]-triazin-8(7H)-one.

Authors:  Long-Chih Hwang; Shin-Yi Jane; Hsing-Yi Lai; Chun-Hsien Tu; Gene-Hsiang Lee
Journal:  Molecules       Date:  2006-06-22       Impact factor: 4.411

6.  Identification by high-throughput screening of viridin analogs as biochemical and cell-based inhibitors of the cell cycle-regulated nek2 kinase.

Authors:  Daniel G Hayward; Yvette Newbatt; Lisa Pickard; Eilis Byrne; Guojie Mao; Samantha Burns; Navdeep K Sahota; Paul Workman; Ian Collins; Wynne Aherne; Andrew M Fry
Journal:  J Biomol Screen       Date:  2010-07-27

7.  Synthesis and anticancer activity of some fused pyrimidines and related heterocycles.

Authors:  S A Al-Issa
Journal:  Saudi Pharm J       Date:  2012-10-24       Impact factor: 4.330

8.  3-Amino-8-hydroxy-4-imino-6-methyl-5-phenyl-4,5-dihydro-3H-chromeno [2,3-d]pyrimidine: an effecient key precursor for novel synthesis of some interesting triazines and triazepines as potential anti-tumor agents.

Authors:  Mohamed G Badrey; Sobhi M Gomha
Journal:  Molecules       Date:  2012-09-27       Impact factor: 4.411
  8 in total

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