Literature DB >> 19615897

Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors.

Mourad Chioua1, Abdelouahid Samadi, Elena Soriano, Olivier Lozach, Laurent Meijer, José Marco-Contelles.   

Abstract

The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kinases [IC(50) (microM) DYRK1A=11; CDK5=0.41; GSK-3=1.5] we have observed that 3,6-diamino-4-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) constitutes a potential new and simple lead compound in the search of drugs for the treatment of Alzheimer's disease.

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Year:  2009        PMID： 19615897     DOI： 10.1016/j.bmcl.2009.06.099

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


  8 in total

1.  Catalyst-free synthesis of quinazolin-4-ones from (hetero)aryl-guanidines: application to the synthesis of pyrazolo[4,3-f]quinazolin-9-ones, a new family of DYRK1A inhibitors.

Authors:  Julien Debray; Simon Bonte; Olivier Lozach; Laurent Meijer; Martine Demeunynck
Journal:  Mol Divers       Date:  2012-09-19       Impact factor: 2.943

2.  Synthesis of multicyclic pyridine and quinoline derivatives via intramolecular C-H bond functionalization.

Authors:  Sirilata Yotphan; Robert G Bergman; Jonathan A Ellman
Journal:  Org Lett       Date:  2010-07-02       Impact factor: 6.005

3.  Consensus models for CDK5 inhibitors in silico and their application to inhibitor discovery.

Authors:  Jiansong Fang; Ranyao Yang; Li Gao; Shengqian Yang; Xiaocong Pang; Chao Li; Yangyang He; Ai-Lin Liu; Guan-Hua Du
Journal:  Mol Divers       Date:  2014-12-16       Impact factor: 2.943

4.  Novel and Potential Small Molecule Scaffolds as DYRK1A Inhibitors by Integrated Molecular Docking-Based Virtual Screening and Dynamics Simulation Study.

Authors:  Mir Mohammad Shahroz; Hemant Kumar Sharma; Abdulmalik S A Altamimi; Mubarak A Alamri; Abuzer Ali; Amena Ali; Safar Alqahtani; Ali Altharawi; Alhumaidi B Alabbas; Manal A Alossaimi; Yassine Riadi; Ahmad Firoz; Obaid Afzal
Journal:  Molecules       Date:  2022-02-09       Impact factor: 4.411

Review 5.  Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's?

Authors:  Breland Smith; Federico Medda; Vijay Gokhale; Travis Dunckley; Christopher Hulme
Journal:  ACS Chem Neurosci       Date:  2012-08-28       Impact factor: 4.418

6.  GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS.

Authors:  Hagit Eldar-Finkelman; Ana Martinez
Journal:  Front Mol Neurosci       Date:  2011-10-31       Impact factor: 5.639

7.  Discovery of the first dual GSK3β inhibitor/Nrf2 inducer. A new multitarget therapeutic strategy for Alzheimer's disease.

Authors:  Isabel Gameiro; Patrycja Michalska; Giammarco Tenti; Ángel Cores; Izaskun Buendia; Ana I Rojo; Nikolaos D Georgakopoulos; Jesús M Hernández-Guijo; María Teresa Ramos; Geoffrey Wells; Manuela G López; Antonio Cuadrado; J Carlos Menéndez; Rafael León
Journal:  Sci Rep       Date:  2017-03-31       Impact factor: 4.379

8.  Catalyst-free synthesis of tetrahydrodipyrazolopyridines via an one-pot tandem and green pseudo-six-component reaction in water.

Authors:  Mina Keihanfar; Bi Bi Fatemeh Mirjalili
Journal:  BMC Chem       Date:  2022-03-04
  8 in total

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