Noguchi Tomomi, Fujimoto Haruka, Sano Hiroko, Miyajima Atsushi, Miyachi Hiroyuki, Hashimoto Yuichi
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Bioorg Med Chem Lett. 2005 Dec 15;15(24):5509-13. doi: 10.1016/j.bmcl.2005.08.086. Epub 2005 Sep 23.
5-Hydroxy-2-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33: 10), which was obtained during our previous structural development studies on thalidomide, was revealed to possess potent anti-angiogenic activity in a human umbilical vein endothelial cell (HUVEC) assay. Thalidomide (1) and its metabolite, 5-hydroxythalidomide (5-HT: 2), which possesses a hydroxyl group at the position corresponding to that of 5HPP-33, as well as IMiDs (immunomodulatory derivatives of thalidomide: 3 and 5), also showed weak or moderate activity in the same assay.
5-羟基-2-(2,6-二异丙基苯基)-1H-异吲哚-1,3-二酮（5HPP-33: 10）是我们之前在沙利度胺结构开发研究过程中获得的，在人脐静脉内皮细胞（HUVEC）试验中显示出强大的抗血管生成活性。沙利度胺（1）及其代谢物5-羟基沙利度胺（5-HT: 2），其在与5HPP-33相应的位置具有一个羟基，以及免疫调节剂（沙利度胺的免疫调节衍生物：3和5），在同一试验中也显示出弱或中等活性。
