期刊
ADVANCED SYNTHESIS & CATALYSIS
卷 357, 期 1, 页码 83-87出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201400993
关键词
alkaloids; antitumor agents; asymmetric synthesis; drug design; heterocycles
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
- Ontario Partnership for Innovation and Commercialization (OPIC)
- Advanced Biomanufacturing Centre (Brock University)
The first active aza analogue of narciclasine was synthesized from a pentasubstituted derivative of nicotinic acid. The key features of the synthesis include a halogen dance of bromopyridine and an intramolecular Heck reaction with a conduramine derived chemoenzymatically from bromobenzene. 10-Aza-narciclasine was found to have reasonable activity against several cancer cell lines.
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