期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 4, 页码 1519-1540出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01407
关键词
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资金
- National Natural Science Foundation of China [81273364, 81773114, 91213303]
- Shenzhen Salubris Pharmaceuticals Co., Ltd.
Salutaxel (3) is a conjugate of docetaxel (7) and a muramyl dipeptide (MDP) analogue. Docetaxel (7) has been recognized as a highly active chemotherapeutic agent against various cancers. MDP and its analogues are powerful potentiators of the antitumor actions of various tumor-necrotizing agents. This article documents the discovery of compound 3 and presents pharmacological proof of its biological function in tumor-bearing mice. Drug candidate 3 was superior to compound 7 in its ability to prevent tumor growth and metastasis. Compound 3 suppressed myeloid-derived suppressor cell (MDSC) accumulation in the spleens of tumor-bearing mice and decreased various serum inflammatory cytokines levels. Furthermore, compound 3 antagonized the nucleotide-binding oligomerization domain-like receptor 1 (NOD1) signaling pathway both in vitro and in vivo.
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