Synthesis and biological evaluation of simplified ajudazol derivatives reveal potent 5-lipoxygenase inhibition and considerable apoptotic activity in neuroblastoma cells

被引：1
|
作者：
Wollnitzke, Philipp [1 ]
Wagner, Raphael [1 ]
Afsar, Sumaiya Yasmeen [2 ]
Werner, Markus [3 ]
Geschold, Robin [4 ]
Mueller, Christa E. [4 ]
Werz, Oliver [3 ]
van Echten-Deckert, Gerhild [2 ]
Menche, Dirk [1 ]
机构：
[1] Univ Bonn, Kekule Inst Organ Chem & Biochem, Gerhard Domagk Str 1, D-53121 Bonn, Germany
[2] Univ Bonn, Biochem Kekule Inst, Inst Membrane Biol & Lipid, Life & Med Sci LIMES, D-53121 Bonn, Germany
[3] Friedrich Schiller Univ Jena, Inst Pharm, Dept Pharmaceut & Med Chem, Philosophenweg 14, D-07743 Jena, Germany
[4] Univ Bonn, Pharmaceut Inst, Dept Pharmaceut & Med Chem, Immenburg 4, D-53121 Bonn, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2023年 / 94卷
关键词：
Ajudazol; Derivative; Anti -inflammatory activity; Neuroblastoma cells; CHONDROMYCES-CROCATUS; ALKYNES;
D O I：
10.1016/j.bmcl.2023.129464
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Simplified analogues of the myxobacterial polyketide ajudazol were obtained by synthesis and evaluated for their biological activities. Potent simplified 5-lipoxygenase inhibitors were identified. Moreover, strong anti -proliferative and apoptotic activities were observed in brain cancer cell lines at low nano-to micromolar concentrations.
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页数：4
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