Tubulin-polymerization inhibitors derived from thalidomide.
2-(2,6-Diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione (5HPP-33), which was obtained during our previous structural development studies on thalidomide, was revealed to possess potent tubulin-polymerization-inhibiting activity, comparable to that of the known tubulin-polymerization inhibitors, rhizoxin and colchicine. A major metabolite of thalidomide, 5-hydroxythalidomide, which possesses a hydroxyl group at the position corresponding to that of 5HPP-33, also showed moderate inhibitory activity.
Inatsuki
Shunsuke
S
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
Oda
Sawako
S
Iguchi
Toyotaka
T
Kizaki
Masahiro
M
Hashimoto
Yuichi
Y
Kobayashi
Hisayoshi
H
D003078:Colchicine / Q000494:pharmacology; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D054833:Isoindoles; D007783:Lactones / Q000494:pharmacology; D018942:Macrolides; D009419:Nerve Tissue Proteins / Q000737:chemistry* / Q000494:pharmacology; D013792:Thalidomide / Q000737:chemistry*; D013997:Time Factors; D014404:Tubulin / Q000378:metabolism; D050257:Tubulin Modulators
C501339:2-(2,6-diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione; D007211:Indoles; D054833:Isoindoles; D007783:Lactones; D018942:Macrolides; D009419:Nerve Tissue Proteins; D014404:Tubulin; D050257:Tubulin Modulators; D013792:Thalidomide; C041443:rhizoxin; D003078:Colchicine