2. Academic Validation
  3. Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone

Cytotoxic Michael-type amine adducts of alpha-methylene lactones alantolactone and isoalantolactone

  • Bioorg Med Chem Lett. 2001 Feb 12;11(3):429-31. doi: 10.1016/s0960-894x(00)00686-7.
N J Lawrence 1,  A T McGown,  J Nduka,  J A Hadfield,  R G Pritchard
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PMID: 11212128 DOI: 10.1016/s0960-894x(00)00686-7
Abstract

Two series of cytotoxic (IC50, K562 cell line, 1-24 microM) alpha-aminomethyl substituted lactones 3 and 4 were prepared by stereoselective Michael-type addition of amines to alantolactone (1) and isoalantolactone (2). The lactones 1 and 2 and their amine adducts induce Apoptosis and act as alkylating agents.

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