TY - JOUR
T1 - Antimalarial and cytotoxic activities of bicyclo[6.4.0]dodecenones
AU - Fujishima, H.
AU - Takeshita, H.
AU - Toyota, M.
AU - Kim, H. S.
AU - Wataya, Y.
AU - Tanaka, M.
AU - Sasaki, T.
AU - Ihara, M.
PY - 2001
Y1 - 2001
N2 - 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.
AB - 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.
KW - Antimalarial activity
KW - Bicyclo[6.4.0]dodecenone
KW - Cytotoxicity
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U2 - 10.1248/cpb.49.572
DO - 10.1248/cpb.49.572
M3 - Article
C2 - 11383608
AN - SCOPUS:0034981806
SN - 0009-2363
VL - 49
SP - 572
EP - 575
JO - Chemical and Pharmaceutical Bulletin
JF - Chemical and Pharmaceutical Bulletin
IS - 5
ER -