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    CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE
    2.
    发明公开
    CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE 审中-公开
    双功能共轭物的化学合成及抗肿瘤和抗转移效应

    公开(公告)号：EP3239139A1

    公开(公告)日：2017-11-01

    申请号：EP17175843.6

    申请日：2011-05-27

    申请人： Shenzhen Salubris Pharmaceuticals Co., Ltd

    发明人： LIU, Gang ,  ZHAO, Nan ,  MA, Yao

    IPC分类号： C07D305/14 ,  C07K5/06 ,  A61K31/337 ,  A61P35/00 ,  A61P35/04 ,  A61P37/04 ,  C07D405/12 ,  C07D409/12 ,  A61K47/65 ,  A61K47/54

    摘要： The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as showed by formula I. In detail, 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。具体而言，紫杉醇或多西他赛与胞壁酰二肽衍生物连接形成缀合物，因此双重抗肿瘤和抗 通过化疗和免疫疗法的组合实现了转移的效果。 本发明还公开了紫杉醇或多西紫杉醇和胞壁酰二肽衍生物缀合物通过固相和液相合成的组合来合成，并且所述缀合物可以用于制造抗肿瘤药物，如可靠的生物测定所证明的。