期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 8, 页码 1885-1888出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.022
关键词
Brasilamide E; Synthesis; Derivatives; Selectivity; Cytotoxicity
资金
- National Natural Science Foundation of China [81273395]
- National Program of Drug Research and Development [2012ZX09301-003]
Brasilamide E (1) is a bisabolane sesquiterpenoid isolated from the solid-substrate fermentation cultures of a plant endophytic fungus Paraconiothyrium brasiliense. The compound specifically inhibited proliferation of the MCF-7 cells, but did not show cytotoxicity towards the negative controls HaCaT and NIH3T3 cells (IC50 > 50 mu M). To improve its potency while maintain selectivity, a total of 27 derivatives of 1 were designed, synthesized, and evaluated for in vitro cytotoxicity against six tumor cell lines and the negative control NIH3T3 cells. Among these compounds, compound 12b showed significantly improved potency against the MCF-7, HeLa, and HO8910 cells with IC50 values of 0.13-0.25 mu M compared to 1 (IC50 8.47-18.00 mu M), and remained nontoxic to the NIH3T3 cells. (C) 2016 Elsevier Ltd. All rights reserved.
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