Site-directed late-stage diversification of macrocyclic nannocystins facilitating anticancer SAR and mode of action studies.
RSC MEDICINAL CHEMISTRY(2023)
摘要
Nannocystins are a family of 21-membered cyclodepsipeptides with excellent anticancer activity. However, their macrocyclic architecture poses a significant challenge to structure modification. Herein, this issue is addressed by leveraging the strategy of post-macrocyclization diversification. In particular, a novel serine-incorporating nannocystin was designed so that its appending hydroxyl group could diversify into a wide variety of side chain analogues. Such effort facilitated not only structure-activity correlation at the subdomain of interest, but also the development of a macrocyclic coumarin-labeled fluorescence probe. Uptake experiments indicated good cell permeability of the probe, and endoplasmic reticulum was identified as its subcellular localization site.
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关键词
macrocyclic nannocystins,anticancer sar,site-directed,late-stage
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