Stereospecific Synthesis and Biological Evaluation of Monodesmethyl Metabolites of (+)-13a-(S)-Deoxytylophorinine as Potential Antitumor Agents

Abstract

Three major monodesmethyl metabolites of (+)-13a-(S)-deoxytylophorinine were synthesized stereospecifically and their configurations at C-13a were determined. Biological assays revealed that one of the metabolites, 3-O-desmethyl-13a-(S)-deoxytylophorinine, had a higher cytotoxic potency than the parent compound or the positive controls doxorubicin (Adriamycin) and paclitaxel (Taxol).

Key words

alkaloids - medicinal chemistry - antitumor agents - stereoselective synthesis

• References

• 1 These authors contributed equally to this study.
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