来那度胺及其氨基糖偶联物的合成及抗肿瘤血管生成活性

Synthesis and anti-angiogenesis evaluation of mutual prodrugs of lenalidomide and glucosamines

摘要: 为提高来那度胺对肿瘤组织的靶向性，利用前药原理，通过丁二酰基或戊二酰基将来那度胺与氨基糖进行偶联，设计合成了8个来那度胺和氨基糖偶联物( 4a~4h )，其结构均经IR、¹H NMR、MS、元素分析确证。初步体外实验结果显示化合物 4a~4c 能够抑制血管内皮细胞的增殖。

Abstract: To improve the targeting effect of lenalidomide on cancer cells,eight coupling compounds( 4a-4h ) of lenalidomide and aminosaccharides were designed and synthesizedTheir structures were characterized by IR,¹H NMR,MS and elemental analysisPreliminary biological evaluation results showed that compounds 4a-4c could inhibit HUVEC cell proliferation in vitro.