Total syntheses and structure-activity relationship study of parthenolide analogues

Two new parthenolide analogues were obtained by total synthesis and assayed for their in vitro anticancer activities to study their structure-activity relationship. Based on the structure and anticancer activity results, two new SAR can be drawn: (1) replacement of the lactone moiety with lactam moiety greatly decreased the anticancer activity; (2) the C-14 methyl group of parthenolide might be important for its high anticancer activity.213