Abstract

Alkoxy-substituted 1-aryl-3-(arylamino)prop-2-en-1-ones and 1-aryl-3-(arylamino)but-2en-1-ones were synthesized by the addition of anilines to 1,3-dioxo derivatives or aryl ethynyl ketones. The cis-trans isomerism of these compounds was studied. Biological tests on a sea urchin embryo model showed that 1-aryl-3-(arylamino)prop-2-en-1-ones exhibit an antimitotic effect both via microtubule destabilization and through the action on other cellular targets. The antiproliferative activity of these compounds increases with an increase in the number of alkoxy substituents in 1-aryl ring, whereas the presence of one methoxy group in the para position proved to be optimal for the arylamino moiety.

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