Synthesis of mycalazol and mycalazal analogs with potent antiproliferating activities

Abstract

Four 2,5-disubstituted pyrrole and two 2-disubstituted thiophene analogs of the natural products mycalazol 5 and mycalazal 2 have been prepared using the Stille coupling reaction. All four analogs displayed potent antiproliferating activity against several human cancer cell lines with IC 50 values in the nanomolar range.Scheme 2 Synthesis of mycalazol 5 and mycalazal 11 analogs.Scheme 3 Synthesis of thiophene analogs 18 and 19.