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

Molecules 2019 Nov 10;24(22). Epub 2019 Nov 10.

Faculty of Chemistry, Philipps University Marburg, Hans-Meerwein-Straße 4, 35032 Marburg, Germany.

A series of 2-methoxypyridine-3-carbonitrile (-)-bearing aryl substituents were successfully synthesized in good yields by the condensation of chalcones (-) with malononitrile in basic medium. The condensation process, in most cases, offers a route to a variety of methoxypyridine derivatives (-) 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 and exhibit promising antiproliferative effects (IC 1-5 µM) against those three cancer cell lines.

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http://dx.doi.org/10.3390/molecules24224072DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6891325PMC
November 2019
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