Synthesis and Antitumor Evaluation of a Novel Class of 4-Substituted-1,4-Dihydroisoquinolin-3-ones

An efficient method for the solution-phase parallel synthesis of 4-substituted-1,4-dihydroisoquinolin-3-ones is developed. The isoquinolinones were constructed employing an intramolecular Heck reaction, providing full regio- and stereoselectivity. Most of the synthesized compounds showed potent antiproliferative activities against tumor cell lines.