N-Conjugate prodrugs of galiellalactone

Zilma Escobar,Ritha Gidlöf,Martin Johansson,Rebecka Hellsten,Olov Sterner

Tetrahedron Letters（2016）

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摘要

•The reactivity of galiellalactone toward secondary amines was investigated.•Several amine adducts of galiellalactone were prepared and characterized.•The Michael addition is reversible and the adducts generate galiellalactone.•The stability of the adducts depends on the pH.•The amine adducts are potential prodrugs of galiellalactone.

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关键词

Galiellalactone,Michael addition,Amine prodrug,Prostate cancer,Mechanism investigation

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