Antimalarial and cytotoxic activities of bicyclo[6.4.0]dodecenones

H. Fujishima, H. Takeshita, M. Toyota, H. S. Kim, Y. Wataya, M. Tanaka, T. Sasaki, M. Ihara

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5 Citations (Scopus)

Abstract

Biological evaluations of bicyclo[6.4.0]dodecenone derivatives on antimalarial activity in vitro against Plasmodium falciparum and cytotoxicity against human KB cells were made. (±)-(1R*4S*7R*,8S*)-4-tert- Butyldimethylsiloxy-5,5-dimethyl-1-methyl-9-methylene-7- phenylsulfonylbicyclo[6.4.0]dodec-2,11-dien-10-one (15) exhibited potent antimalarial activity, whereas (±)-(1R*7*8*)-1-methyl-9-methylene-7- phenylsulfonylbicyclo[6.4.0]dodec-2,11-dien-10-one (14) showed significant cytotoxic activity in human KB cells. Both 14 and 15 possess, as a structural character, the exo-methylene moiety in their 6-membered ring of the 8-6 fused ring system.

Original languageEnglish
Pages (from-to)572-575
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume49
Issue number5
DOIs
Publication statusPublished - Jun 15 2001
Externally publishedYes

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Keywords

  • Antimalarial activity
  • Bicyclo[6.4.0]dodecenone
  • Cytotoxicity

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

Cite this

Fujishima, H., Takeshita, H., Toyota, M., Kim, H. S., Wataya, Y., Tanaka, M., Sasaki, T., & Ihara, M. (2001). Antimalarial and cytotoxic activities of bicyclo[6.4.0]dodecenones. Chemical and Pharmaceutical Bulletin, 49(5), 572-575. https://doi.org/10.1248/cpb.49.572