Synthesis and antiproliferative activities of novel quartenary ammonium spinosyn derivatives

[Display omitted] •Thirteen novel quartenary ammonium spinosyn derivatives were synthesized.•Greatly enhanced antiproliferative activities.•Lipophicility has a great influence on the antiproliferative effects of these derivatives.•Compound 11d exhibited remarkably enhanced OXPHS inhibition and apopt...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-11, Vol.28 (20), p.3346-3349
Hauptverfasser:	Ma, Da-You, Wang, Long-Long, Lai, Qin, Peng, Kun-Jian, Li, Xuan, Li, Zeng-Xia, Liu, Li-Jun, Luo, Zhi-Yong, Liu, Su-You
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antiproliferative activity Apoptosis - drug effects Cell Line, Tumor Derivatives Drug Screening Assays, Antitumor Humans Hydrophobic and Hydrophilic Interactions Macrolides - chemical synthesis Macrolides - chemistry Macrolides - pharmacology Mitochondria Mitochondria - metabolism Molecular Structure Oxidative Phosphorylation - drug effects Quaternary Ammonium Compounds - chemical synthesis Quaternary Ammonium Compounds - chemistry Quaternary Ammonium Compounds - pharmacology Respiration Spinosad Structure-Activity Relationship
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