Literature DB >> 28745236

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.

Rafat M Mohareb1, Amr S Abouzied2,3, Nermeen S Abbas4,5.   

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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

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Keywords:  1; 2-aminoprop-1-ene-1; 3-tricarbonitrile; antiproliferative activity.; kinase inhibitors; pyran; pyridine

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Year:  2018        PMID: 28745236     DOI: 10.2174/1871520617666170725153523

Source DB:  PubMed          Journal:  Anticancer Agents Med Chem        ISSN: 1871-5206            Impact factor:   2.505


  1 in total

1.  Synthesis and Aminomethylation of 2-Amino-4-(2-chlorophenyl)-6-(dicyanomethyl)-1,4-dihydropyridine-3,5-dicarbonitrile N-Methylmorpholinium Salt.

Authors:  A O Kurskova; V V Dotsenko; K A Frolov; N A Aksenov; I V Aksenova; B S Krivokolysko; A A Peresypkina; E A Chigorina; S G Krivokolysko
Journal:  Russ J Gen Chem       Date:  2022-06-14       Impact factor: 0.779

  1 in total

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