Synthesis and anticancer activity of polyhydroxylated 18-membered analogue of antimycin A3

A novel polyhydroxylated 18-membered analogue of antimycin A3 was synthesized. Our synthesis commenced with Boc-l-threonine and was achieved by way of one-pot homocoupling/ring-closing olefin metathesis reaction cascade and Sharpless asymmetric dihydroxylation. The analogue exhibited a greater anticancer activity against HeLa cells, breast MDA-MB-231 cells, and prostate PC-3 cells compared to the original antimycin A3.