Design and synthesis of a phenyl C-glycoside derivative of Spliceostatin A and its biological evaluation toward prostate cancer treatment

摘要

We designed and synthesized a novel phenyl C-glycoside analogue of Spliceostatin A, which is potent splicing inhibitor and has anti-cancer activities. We successfully synthesized its right phenyl C-glycoside sugar fragment in shorter steps compared to previous synthetic methods for Spliceostatin A and revealed an appropriate fragment combination with a Julia-coupling reaction. Regarding biological activity, the Ph-C-glycoside analogue of Spliceostatin A showed repressed cell proliferation in three prostate cancer cell lines and suppressed AR-V7 expression. (C) 2019 Elsevier Ltd. All rights reserved.