Synthesis and Anticancer Activity of Novel 9--Substituted Berberine Derivatives.

Berberine is a bioactive isoquinoline alkaloid derived from many plants. Although berberine has been shown to inhibit growth and induce apoptosis of several tumor cell lines, its poor absorption and moderate activity hamper its full therapeutic potential. Here, we describe the synthesis of a series of 9--substituted berberine derivatives with improved antiproliferative and apoptosis-inducing activities.