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

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.