Synthesis of 13-amino telekin derivatives and their cytotoxic activity

Author: Wang Xiujie   Zhang Xiumei   Zheng Beibei   Hu Nan   Xie Weidong   Row Kyungho  

Publisher: Taylor & Francis Ltd

E-ISSN: 1478-6427|29|8|756-763

ISSN: 1478-6419

Source: Natural Product Research, Vol.29, Iss.8, 2015-04, pp. : 756-763

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Abstract

Telekin is a eudesmane sesquiterpene-lactone naturally occurring in many medicinal plants with antitumour and anti-inflammatory activity. In this study, a series of 13-amino derivatives of telekin have been synthesised through Michael addition reaction, and their relative configurations were exemplified by the single crystal X-ray diffraction of the dimethylamine adduct. The in vitro cytotoxicity against three tumour cell lines of these amine derivatives was evaluated. The piperidine and 4-hydroxypiperidine adducts displayed stronger cytotoxic activity than telekin.