The present invention provides substituted berbines, processes for the synthesis of substituted berbine compounds preferably through a Bischler-Napieralski cyclization followed by reduction, as well as intermediates used in the synthesis of substituted berbine compounds. The amide precursor for the Bischler-Napieralski reaction could be obtained treating the free amine with acid halides, formate sources or aldehydes. Also provided are methods for using the substituted berbines to inhibit cancer cell growth.