Synthesis 2012; 44(24): 3757-3764
DOI: 10.1055/s-0032-1316810
paper
© Georg Thieme Verlag Stuttgart · New York

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

Pengfei Yu
,
Haining Lv
,
Chao Li
,
Jinhong Ren
,
Shuanggang Ma
,
Song Xu
,
Xiaoguang Chen
,
Shishan Yu*
Further Information

Publication History

Received: 09 September 2012

Accepted after revision: 24 October 2012

Publication Date:
09 November 2012 (online)


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).

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