4.8 Article

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

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ORGANIC LETTERS
卷 14, 期 5, 页码 1290-1293

出版社

AMER CHEMICAL SOC
DOI: 10.1021/ol300182r

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资金

  1. Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan
  2. Uehara Memorial Foundation
  3. Society of Synthetic Organic Chemistry, Japan (Meiji Seika Award in Synthetic Organic Chemistry, Japan)
  4. Suntory Institute for Bioorganic Research (SUNBOR)
  5. Grants-in-Aid for Scientific Research [23102014, 21510221, 23310148] Funding Source: KAKEN

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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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