芳基化诺维霉素类似物的合成与生物评价作为 HSP90 抑制剂。
Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors.
机构信息
Department of Medicinal Chemistry, The University of Kansas, Lawrence, KS 66045-7563, USA.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7170-4. doi: 10.1016/j.bmcl.2011.09.073. Epub 2011 Oct 1.
Abstract
Novobiocin analogs lacking labile glycosidic ether have been designed, synthesized and evaluated for Hsp90 inhibitory activity. Replacement of the synthetically complex noviose sugar with simple aromatic side chains produced analogs that maintain moderate cytotoxic activity against MCF7 and SkBR3 breast cancer cell-lines. Rationale for the preparation of des-noviose novobiocin analogs in addition to their synthesis and biological evaluation are presented herein.
摘要
已设计、合成并评估了缺乏不稳定糖苷醚的新生霉素类似物的热休克蛋白 90（Hsp90）抑制活性。用简单的芳族侧链替代合成复杂的新戊糖，得到了对 MCF7 和 SkBR3 乳腺癌细胞系具有中等细胞毒性的类似物。本文介绍了除合成和生物评价外，还制备去新戊糖新生霉素类似物的理由。
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