Design, Synthesis, and Biological Evaluations of Aplyronine A–Mycalolide B Hybrid Compound

Design, Synthesis, and Biological Evaluations of Aplyronine A–Mycalolide B Hybrid Compound

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 cyt...

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Veröffentlicht in:Organic letters 2012-03, Vol.14 (5), p.1290-1293
Hauptverfasser: Kobayashi, Kenichi, Fujii, Yusuke, Hirayama, Yuichiro, Kobayashi, Shinichi, Hayakawa, Ichiro, Kigoshi, Hideo
Format: Artikel
Sprache:eng
Schlagworte:
Cell Survival - drug effects
Drug Design
HeLa Cells
Humans
Macrolides - chemical synthesis
Macrolides - pharmacology
Models, Molecular
Molecular Structure
Oxazoles - chemical synthesis
Oxazoles - pharmacology
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Zusammenfassung: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol300182r