Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids.

: The archazolids represent potent antiproliferative compounds which have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply render the development of more readily available analogs of high importance. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives revealing important structure-activity relationship data and insights into the pharmacophore of these complex polyketides.