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ID: ALA5252546
Journal: J Med Chem
Title: Salutaxel, a Conjugate of Docetaxel and a Muramyl Dipeptide (MDP) Analogue, Acts as Multifunctional Prodrug That Inhibits Tumor Growth and Metastasis.
Authors: Wen X, Zheng P, Ma Y, Ou Y, Huang W, Li S, Liu S, Zhang X, Wang Z, Zhang Q, Cheng W, Lin R, Li H, Cai Y, Hu C, Wu N, Wan L, Pan T, Rao J, Bei X, Wu W, Jin J, Yan J, Liu G.
Abstract: 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.
CiteXplore: 29357251