Total Synthesis of Stipiamide and Designed Polyenes as New Agents for the Reversal of Multidrug Resistance

摘要

The synthesis of (-)-stipiamide (1) is reported together with the designed enynes 2 (6,7-dehydrostipiamide) and 3 that are now shown to reverse the multidrug resistance (MDR) of human breast cancer cells (MCF-7adrR). Stipiamide was assembled using a Stille coupling with (E)-vinyl iodide 17 and (Z)-stannyl amide 16 in 78/100 yield.