Design, synthesis, and biological evaluations of aplyronine A-mycalolide B hybrid compound

Kenichi Kobayashi; Yusuke Fujii; Yuichiro Hirayama; Shinichi Kobayashi; Ichiro Hayakawa; Hideo Kigoshi

doi:10.1021/ol300182r

Design, synthesis, and biological evaluations of aplyronine A-mycalolide B hybrid compound

Kenichi Kobayashi, Yusuke Fujii, Yuichiro Hirayama, Shinichi Kobayashi, Ichiro Hayakawa, Hideo Kigoshi

Faculty of Engineering

Research output: Contribution to journal › Article › peer-review

27 Citations (Scopus)

Abstract

A hybrid compound consisting of aplyronine A and mycalolide B was synthesized, and its biological activities were evaluated. The hybrid compound was found to have somewhat more potent actin-depolymerizing activity than aplyronine A. In contrast, the hybrid compound possessed about 1000-fold less cytotoxicity than aplyronine A. These results indicated that there is no direct correlation between actin-depolymerizing activity and cytotoxicity.

Original language	English
Pages (from-to)	1290-1293
Number of pages	4
Journal	Organic Letters
Volume	14
Issue number	5
DOIs	https://doi.org/10.1021/ol300182r
Publication status	Published - Mar 2 2012

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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10.1021/ol300182r

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abstract = "A hybrid compound consisting of aplyronine A and mycalolide B was synthesized, and its biological activities were evaluated. The hybrid compound was found to have somewhat more potent actin-depolymerizing activity than aplyronine A. In contrast, the hybrid compound possessed about 1000-fold less cytotoxicity than aplyronine A. These results indicated that there is no direct correlation between actin-depolymerizing activity and cytotoxicity.",

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AU - Kobayashi, Kenichi

AU - Fujii, Yusuke

AU - Hirayama, Yuichiro

AU - Kobayashi, Shinichi

AU - Hayakawa, Ichiro

AU - Kigoshi, Hideo

PY - 2012/3/2

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N2 - A hybrid compound consisting of aplyronine A and mycalolide B was synthesized, and its biological activities were evaluated. The hybrid compound was found to have somewhat more potent actin-depolymerizing activity than aplyronine A. In contrast, the hybrid compound possessed about 1000-fold less cytotoxicity than aplyronine A. These results indicated that there is no direct correlation between actin-depolymerizing activity and cytotoxicity.

AB - A hybrid compound consisting of aplyronine A and mycalolide B was synthesized, and its biological activities were evaluated. The hybrid compound was found to have somewhat more potent actin-depolymerizing activity than aplyronine A. In contrast, the hybrid compound possessed about 1000-fold less cytotoxicity than aplyronine A. These results indicated that there is no direct correlation between actin-depolymerizing activity and cytotoxicity.

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Design, synthesis, and biological evaluations of aplyronine A-mycalolide B hybrid compound

Abstract

ASJC Scopus subject areas

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