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Synthesis and biological evaluation of unnatural derivatives of narciclasine: 7- aza-narciclasine and its N-oxide

机译:水仙子碱非天然衍生物7-氮杂-水仙子碱及其N-氧化物的合成及生物学评价

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摘要

Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to construct the carbostyryl ring system. The compounds were submitted to biological screening against cancer cell lines. Full experimental and spectra data are provided for all new compounds.
机译:制备了几种非天然的水杨酸衍生物,其中的C-7碳被氮取代。 7-氮杂衍生物及其N-氧化物是通过碘代吡啶甲酸与化学上衍生自溴苯的conduramine单元偶联而制得的。分子内Heck反应用于构建羧甲基苯乙烯环系统。将该化合物进行针对癌细胞系的生物筛选。提供了所有新化合物的完整实验数据和光谱数据。

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