公开(公告)号：US08686187B2

公开(公告)日：2014-04-01

申请号：US13124504

申请日：2009-10-15

申请人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

发明人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

IPC分类号： C07C233/05 ,  C07C217/84 ,  C07C237/20 ,  C07C231/08 ,  C07C213/02

CPC分类号： A61K31/09 ,  A61K31/165 ,  A61K31/661 ,  C07C217/84 ,  C07C237/04 ,  C07F9/12

摘要： 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.

摘要翻译： 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苯乙醚B芳环的4'位通过乙氧基化学改性，3'位的羟基同时修饰为水溶性前药，如磷酸盐，类似地，氨基酸侧 链引入3'位的氨基，形成具有式（I）结构的氨基酰胺水溶性前药，乙氧基二苯乙烷衍生物及其前药包括强大的微管蛋白聚集抑制能力和对肿瘤血管具有明显的靶损伤作用，有选择地引起 功能障碍和肿瘤血管结构损伤，并诱导血管内皮细胞凋亡，以发挥肿瘤细胞杀伤作用或抑制肿瘤转移的作用，以免肿瘤细胞不受营养和氧气的支持。

公开(公告)号：US20120046492A1

公开(公告)日：2012-02-23

申请号：US13124504

申请日：2009-10-15

申请人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

发明人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

IPC分类号： C07C43/23 ,  C07F9/12 ,  C07C231/08 ,  C07C41/30 ,  C07C213/02 ,  C07C217/84 ,  C07C237/20

CPC分类号： A61K31/09 ,  A61K31/165 ,  A61K31/661 ,  C07C217/84 ,  C07C237/04 ,  C07F9/12

摘要： 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.

摘要翻译： 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苯乙醚B芳环的4'位通过乙氧基化学改性，3'位的羟基同时修饰为水溶性前药，如磷酸盐，类似地，氨基酸侧 链引入3'位的氨基，形成具有式（I）结构的氨基酰胺水溶性前药，乙氧基二苯乙烷衍生物及其前药包括强大的微管蛋白聚集抑制能力和对肿瘤血管具有明显的靶损伤作用，有选择地引起 功能障碍和肿瘤血管结构损伤，并诱导血管内皮细胞凋亡，以发挥肿瘤细胞杀伤作用或抑制肿瘤转移的作用，以免肿瘤细胞不受营养和氧气的支持。