title: Synthesis of 13-amino telekin derivatives and their cytotoxic activity.
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.
authors.affiliation: a Department of Pharmacy , College of Marine Science, Shandong University , Weihai 264209 , P.R. China.
authors.forename: Xiujie
authors.initials: X
authors.lastname: Wang
authors.forename: Xiumei
authors.initials: X
authors.lastname: Zhang
authors.forename: Beibei
authors.initials: B
authors.lastname: Zheng
authors.forename: Nan
authors.initials: N
authors.lastname: Hu
authors.forename: Weidong
authors.initials: W
authors.lastname: Xie
authors.forename: Kyungho
authors.initials: K
authors.lastname: Row
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry; D045787:Sesquiterpenes, Eudesmane / Q000138:chemical synthesis* / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045787:Sesquiterpenes, Eudesmane; C584237:telekin
keywords: Michael addition reaction; cytotoxicity; eudesmane; sesquiterpene lactone; telekin