申请人:Wu Fanhong
公开号:US20120046492A1
公开(公告)日:2012-02-23
The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4′ position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3′ thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3′ to form amino acid amide water soluble prodrug having the structure shown as formula (I)
the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.
本发明公开了一种乙氧基二苯乙烷衍生物及其合成方法和用途。通过在苯乙烷B芳环的4'位进行乙氧基化学修饰,并同时将3'位的羟基修饰为水溶性前药,如磷酸盐,类似地,将氨基酸侧链引入到3'位的氨基上形成氨基酸酰胺水溶性前药,其结构如式(I)所示。该乙氧基二苯乙烷衍生物及其前药具有强大的微管凝聚抑制能力和明显的靶向损伤作用于肿瘤血管,选择性地引起肿瘤血管的功能障碍和结构损伤,并诱导血管内皮细胞凋亡,以发挥杀灭肿瘤细胞或抑制肿瘤转移的作用,当肿瘤细胞没有营养和氧气的支持时。