| Autor: |
Wen, Xiaoming, Zheng, Purong, Ma, Yao, Ou, Yingye, Huang, Weixin, Li, Shuo, Liu, Shoujia, Zhang, Xuan, Wang, Ziyu, Zhang, Qianli, Cheng, Wenming, Lin, Ruwen, Li, Hongzu, Cai, Youyou, Hu, Chunyun, Wu, Ningbin, Wan, Long, Pan, Tingting, Rao, Jinlong, Bei, Xuelu, Wu, Weibin, Jin, Jian, Yan, Jie, Liu, Gang |
| Zdroj: |
Journal of Medicinal Chemistry; 20240101, Issue: Preprints |
| Abstrakt: |
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 3and presents pharmacological proof of its biological function in tumor-bearing mice. Drug candidate 3was superior to compound 7in its ability to prevent tumor growth and metastasis. Compound 3suppressed myeloid-derived suppressor cell (MDSC) accumulation in the spleens of tumor-bearing mice and decreased various serum inflammatory cytokines levels. Furthermore, compound 3antagonized the nucleotide-binding oligomerization domain-like receptor 1 (NOD1) signaling pathway both in vitro and in vivo. |
| Databáze: |
Supplemental Index |
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