TY - JOUR
T1 - Tubulin-polymerization inhibitors derived from thalidomide
AU - Inatsuki, Shunsuke
AU - Noguchi, Tomomi
AU - Miyachi, Hiroyuki
AU - Oda, Sawako
AU - Iguchi, Toyotaka
AU - Kizaki, Masahiro
AU - Hashimoto, Yuichi
AU - Kobayashi, Hisayoshi
N1 - Funding Information:
The work described in this paper was partially supported by Grants-in-Aid for Scientific Research from the Ministry of Education, Culture, Sports, Science, and Technology, Japan, and the Japan Society for the Promotion of Science.
PY - 2005/1/17
Y1 - 2005/1/17
N2 - 2-(2,6-Diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione (5HPP-33), has potent tubulin-polymerization-inhibiting activity. A metabolite of thalidomide, 5-hydroxythalidomide (2) also showed moderate inhibitory activity 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.
AB - 2-(2,6-Diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione (5HPP-33), has potent tubulin-polymerization-inhibiting activity. A metabolite of thalidomide, 5-hydroxythalidomide (2) also showed moderate inhibitory activity 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.
KW - Inhibitor
KW - Polymerization
KW - Thalidomide
KW - Tubulin
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U2 - 10.1016/j.bmcl.2004.10.072
DO - 10.1016/j.bmcl.2004.10.072
M3 - Article
C2 - 15603947
AN - SCOPUS:10644269779
SN - 0960-894X
VL - 15
SP - 321
EP - 325
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 2
ER -