庚烷
苯
亲脂性
化学
等甾体
戒指(化学)
溶解度
立体化学
药物化学
有机化学
作者
Pavel K. Mykhailiuk,Dmitry Dibchak
标识
DOI:10.1002/anie.202505519
摘要
3‑Oxabicyclo[3.1.1]heptanes were designed as saturated isosteres of meta‐benzene. Crystallographic analysis revealed that these structures and meta‐benzene have identical geometric properties. Replacement of the central benzene ring in the anticancer drug Sonidegib with 3‐oxabicyclo[3.1.1]heptane provided a patent‐free analogue with a nanomolar potency, reduced lipophilicity and improved water solubility (>500%).
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