期刊
TETRAHEDRON
卷 68, 期 13, 页码 2759-2764出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.02.016
关键词
(-)-Jorumycin; Tetrahydroisoquinoline; Synthesis; Cytotoxicity
资金
- National Natural Science Foundation of China [30672518]
- Specialized Research Fund for the Doctoral Program of Higher Education [20060023025]
(-)-Jorumycin and its 15 C-22 analogues were prepared employing L-tyrosine as the chiral starting material via 21 steps. These analogues, along with (-)-jorumycin itself, were evaluated in vitro for cytotoxicity against HCT-8, BEL-7402, Ketr3, A2780, MCF-7, A549, BGC-823, Hela, HELF, and KB cells. The IC50 values of the cytotoxicity of most of these analogs were at the level of nM, which was similar to that of (-)-jorumycin. Among these analogs including (-)-jorumycin, hippuric acid ester derivative 23 exhibited the most potent and broad-spectrum cytotoxic activity against the ten cell lines with an average IC50 of 2.12 nM. (C) 2012 Elsevier Ltd. All rights reserved.
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