Concise Total Synthesis of Cruentaren A

摘要

Bioassay-guided fractionation of the fermentation broth of the myxobacterium Byssovorax cruenta led to the discovery of the benzolactone cruentaren A (1) and its ring-contracted congener cruentaren B (2).While 2 is largely inactive,1 exhibits pronounced antifungal activity and remarkable cytotoxicity against a panel of human cancer cell lines,with IC50 values in the (sub)nanomolar range,including the multidrug-resistant KB-V1 cell line,for which an IC50 value of 0.6 mg mL-1 has been reported.