公开(公告)号：US20130143826A1

公开(公告)日：2013-06-06

申请号：US13699869

申请日：2011-05-27

申请人： Gang Liu ,  Nan Zhao ,  Yao Ma

发明人： Gang Liu ,  Nan Zhao ,  Yao Ma

IPC分类号： C07K5/02

CPC分类号： C07K5/0215 ,  A61K31/337 ,  A61K47/54 ,  A61K47/542 ,  A61K47/65 ,  C07D305/14 ,  C07D405/12 ,  C07D409/12

摘要： The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

摘要翻译： 本发明公开了如式I所示的双功能缀合物的化学合成，抗肿瘤和抗转移作用。具体地，紫杉醇或多西紫杉醇与胞壁酰二肽衍生物连接以形成缀合物，因此双重抗肿瘤和抗 - 通过化学疗法和免疫治疗联合实现转移效应。 本发明还公开了通过固相和溶液相合成的方法合成紫杉醇或多西他赛和胞壁酰二肽衍生物缀合物，并且所述缀合物可用于制造抗肿瘤药物，如通过可靠的生物测定证明的。