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Natural Product Research
Formerly Natural Product Letters
Volume 29, 2015 - Issue 8
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Articles

Synthesis of 13-amino telekin derivatives and their cytotoxic activity

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Pages 756-763 | Received 08 Sep 2014, Accepted 06 Nov 2014, Published online: 11 Dec 2014
 

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.

Additional information

Funding

This work was partly supported by the Basic Science Research Program of National Research Foundation from the Ministry of Education, Science and Technology of Korea [grant number 2014-002046]. Dr Xie also thanks for the support of the International Scholar Exchange Fellowship Program [grant number ISEF 2014-2015] from the Korea Foundation for Advanced Studies.

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