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.

引用

页数：4

共 30 条

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