Effects of Immunomodulatory Derivatives of Thalidomide (IMiDs) and Their Analogs on Cell-Differentiation, Cyclooxygenase Activity and Angiogenesis
作者:Haruka Fujimoto、Tomomi Noguchi、Hisayoshi Kobayashi、Hiroyuki Miyachi、Yuichi Hashimoto
DOI:10.1248/cpb.54.855
日期:——
Various analogs of known immunomodulatory derivatives of thalidomide (1) (IMiDs: 3, 5) were synthesized, focusing on cell-differentiation-inducing, cyclooxygenase-inhibitory and anti-angiogenesis activities. Among the prepared compounds, NIDO-33 (14) showed cell differentiation-inducing activity on HL-60 cells and anti-angiogenic activity on human umbilical vein endothelial cells (HUVEC). AIDO-00 (7) also showed anti-angiogenic activity. NIDO-11 (8) showed an enhancing effect on all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation, and AIDO-30 (13) exhibited cyclooxygenase (COX)-inhibitory activity.
研究人员合成了沙利度胺(1)的多种已知免疫调节衍生物类似物(IMiDs:3、5),重点研究其细胞分化诱导、环氧化酶抑制和抗血管生成活性。在制备的化合物中,NIDO-33(14)对 HL-60 细胞具有细胞分化诱导活性,对人脐静脉内皮细胞(HUVEC)具有抗血管生成活性。AIDO-00 (7) 也具有抗血管生成活性。NIDO-11(8)对全反式维甲酸(ATRA)诱导的HL-60细胞分化具有增强作用,而AIDO-30(13)则具有抑制环氧化酶(COX)的活性。