Design, synthesis and antiproliferative activity of two new heteroannelated (−)-muricatacin mimics

Two new (−)-muricatacin mimics bearing a furano-furanone ring and an oxygen isostere in the side chain have been designed and synthesized and their in vitro antiproliferative activity was evaluated against several human tumour cell lines. Both analogues showed an increased activity against HL-60 cells with 17- and 185-fold higher potency than (−)-muricatacin. A straightforward synthesis of (−)-muricatacin is also disclosed.

(−)-Muricatacin (1) and the related mimics 3 and 4 have been synthesized and evaluated for their in vitro antitumour activity.Figure optionsDownload as PowerPoint slide