Design and Synthesis of 1,2-Deoxy-pyranose Derivatives of Spliceostatin A Toward Prostate Cancer Treatment

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2020 Jun 20

PMID 32551017

Citations 10

Authors

Yusuke Yoshikawa

Airi Ishibashi

Tsunayoshi Takehara

Takeyuki Suzuki

Kenichi Murai

Yasufumi Kaneda

Keisuke Nimura

Mitsuhiro Arisawa

Affiliations

Soon will be listed here.

Abstract

We designed and synthesized a novel 1,2-deoxy-pyranose and terminal epoxide methyl substituted derivatives of spliceostatin A using Julia-Kocienski olefination as a key step. With respect to the biological activity, the 1,2-deoxy-pyranose analogue of spliceostatin A suppressed AR-V7 expression at the nano level (IC = 3.3 nM). In addition, the toxicity test showed that the 1,2-deoxy-pyranose analogue was able to avoid severe toxicity compared to spliceostatin A.

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