期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 16, 页码 4750-4752出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.068
关键词
Intramolecular aziridine opening; Amaryllidaceae alkaloids; Pancratistatin analogs; Anti-cancer activity
资金
- Natural Sciences and Engineering Research Council of Canada (NSERC)
- Canada Research Chair Program
- Canada Foundation for Innovation (CFI)
- TDC Research, Inc.
- TDC Research Foundation
- Brock University
- National Institutes of Health [P20 RR016480]
The synthesis of two C-1 analogues of pancratistatin has been accomplished in 17 steps from bromobenzene. The key steps involved the enzymatic dihydroxylation, regioselective opening of epoxyaziridine 9 with the alane derived from 8, a solid-state silica-gel-catalyzed intramolecular opening of aziridine to produce phenanthrene 13 whose oxidative cleavage and recyclization provided the full skeleton of the Amaryllidaceae constituents. The new analogues 5 and 6 exhibited promising activity in several human cancer cell lines. (C) 2011 Elsevier Ltd. All rights reserved.
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