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Synthesis of Pyridine and Spiropyridine Derivatives Derived from 2-aminoprop- 1-ene-1,1,3-tricarbonitrile Together with their c-Met Kinase and Antiproliferative Evaluations

[ Vol. 17 , Issue. 14 ]

Author(s):

Rafat M. Mohareb*, Amr S. Abouzied and Nermeen S. Abbas   Pages 1951 - 1962 ( 12 )

Abstract:


Background: Among a wide range of pyridines, 3-cyanopyridines acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the pyridine nucleus were known in the market.

Objective: The aim of this work was to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. To achieve this goal, our strategy was to synthesize a series of 3-cyanopyridine derivatives using 2-aminoprop-1-ene-1,1,3-tricarbonitrile (1) as the key starting material for many heterocyclization reactions.

Method: Muticoponent reactions were adopted using compound 1 to get different pyridine derivatives that were capable for different heterocyclization reactions.

Results: Antiproliferative evaluations and c-Met kinase, Pim-1 kinse inhibitions were perform where some compounds gave high activities.

Conclusion: Compounds that showed high antiprolifeative activity were tested gor c-Met-independent and the results showed that compounds 5c, 5e, 5f, 7c, 7f and 16d were more active than foretinib. The Pim-1 kinase inhibition activity of some selected compounds showed that compounds 5e and 16c were high potent to inhibit Pim-1 activity.

Keywords:

2-aminoprop-1-ene-1, 1, 3-tricarbonitrile, pyran, pyridine, kinase inhibitors, antiproliferative activity.

Affiliation:

Department of Chemistry, Faculty of Science, Cairo University, Giza, Department of Pharmaceutical Chemistry, College of Pharmacy, University of Hail, Hail, Department of Chemistry, Faculty of Science, Taibah University

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