Synthesis and cytotoxicity evaluation of fluorinated brusatol, bruceosin, and dehydrobrusatol

Abstract

Three fluorinated quassinoid analogues—4α-fluorobruceosin, 1α-fluorobrusatol, and 1-fluorodehydrobrusatol—were synthesized from brusatol, bruceosin, and dehydrobrusatol, respectively, by treatment with Selectfluor. These analogues were less cytotoxic to HL-60 cells than their non-fluorinated counterparts.

Keywords

• Brusatol
• Quassinoid
• Semi-synthesis
• Fluoro analogue
• Cytotoxicity