SMALL MOLECULE CONJUGATES SPECIFICALLY ACTIVATED IN TUMOR MICROENVIROMENT FOR TARGETING AND USE THEREOF
申请人:Yafei Shanghai Biolog Medicine Science & Technolog Co., Ltd.
公开号:US20170266308A1
公开(公告)日:2017-09-21
Provided is an anticancer compound including a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R
1
is a normal functional group or a protection group; R
2
is Ala, Thr, Val or Ile; R
3
is Ala, Val or Asn; R
4
is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R
4
H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.