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RSS FeedsMolecules, Vol. 24, Pages 4072: The Synthesis, Characterization, Cytotoxic Activity Assessment and Structure-Activity Relationship of 4-Aryl-6-(2,5-dichlorothiophen-3-yl)-2-methoxypyridine-3-carbonitriles (Molecules)

 
 

10 november 2019 18:00:22

 
Molecules, Vol. 24, Pages 4072: The Synthesis, Characterization, Cytotoxic Activity Assessment and Structure-Activity Relationship of 4-Aryl-6-(2,5-dichlorothiophen-3-yl)-2-methoxypyridine-3-carbonitriles (Molecules)
 




A series of 2-methoxypyridine-3-carbonitrile (5a–i)-bearing aryl substituents were successfully synthesized in good yields by the condensation of chalcones (4a–i) with malononitrile in basic medium. The condensation process, in most cases, offers a route to a variety of methoxypyridine derivatives (6a–g) as side products in poor yields. All new compounds were fully characterized using different spectroscopic methods. Mass ESI-HMRS measurements were also performed. Furthermore, these compounds were screened for their in vitro cytotoxicity activities against three cancer cell lines; namely, those of the liver (line HepG2), prostate (line DU145) and breast (line MBA-MB-231). The cytotoxicity assessment revealed that compounds 5d, 5g, 5h and 5i exhibit promising antiproliferative effects (IC50 1–5 µM) against those three cancer cell lines.


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79 viewsCategory: Biochemistry, Chemistry, Molecular Biology
 
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Molecules, Vol. 24, Pages 4071: ?-Glucosidase and Pancreatic Lipase Inhibitory Activities of Diterpenes from Indian Mango Ginger (Curcuma amada Roxb.) and Its Derivatives (Molecules)
 
 
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