Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide.
4,7-Difluoro-2-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione [4,7FPP-33 (14)] has a potent tubulin-polymerization-inhibiting activity comparable with those of the known tubulin-polymerization inhibitors rhizoxin and colchicine. The structure-activity relationship for fluorine substitution was elucidated.
Yanagawa
Tomonori
T
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Noguchi
Tomomi
T
Miyachi
Hiroyuki
H
Kobayashi
Hisayoshi
H
Hashimoto
Yuichi
Y
D005461:Fluorine / Q000737:chemistry*; D015394:Molecular Structure; D010797:Phthalimides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000378:metabolism*
D010797:Phthalimides; D014404:Tubulin; C037431:phthalimide; D005461:Fluorine