N-Conjugate prodrugs of galiellalactone

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Abstract

A series of amine adducts of the fungal metabolite galiellalactone (1) were prepared by reacting galiellalactone with different secondary amines via a Lewis acid catalyzed Michael addition. The adducts were assayed for in vitro effects toward prostate cancer cell lines and found to possess a similar ability to inhibit cell proliferation as galiellalactone itself. It was found that the Michael addition of amines to 1 is a reversible reaction, releasing 1 at different rates depending on the conditions, and that the adducts are potential prodrugs of galiellalactone. The chemical stability of the amine adducts is especially sensitive to pH, increasing at a lower pH.

Detaljer

Författare
Enheter & grupper
Externa organisationer
  • Glactone Pharma AB
Forskningsområden

Ämnesklassifikation (UKÄ) – OBLIGATORISK

  • Biokemi och molekylärbiologi
  • Cancer och onkologi

Nyckelord

Originalspråkengelska
Sidor (från-till)4090-4093
Antal sidor4
TidskriftTetrahedron Letters
Volym57
Utgivningsnummer36
StatusPublished - 2016 sep 7
PublikationskategoriForskning
Peer review utfördJa