Synthesis and antitumor activity of cyclodepsipeptide zygosporamide and its analogues
AbstractThe synthesis and structure–activity relationships of zygosporamide, a known potent and selective cytotoxic natural product against SF-268 and RXF 393 cell lines, are described. The potencies of the synthetic zygosporamide are similar to those reported for the natural product toward all cancer cell lines examined with the exception of SF-268, the underlying cause of which remains to be elucidated. 恭喜 and 羡慕啊 Welcome new QM from Fudan Univ.
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文章题目 Synthesis of chiral cyclohexane-backbone P,N-ligands derived from pyridine and their applications in asymmetric catalysis
期刊名 Tetrahedron Letters
年份，卷（期），起止页码 2007, 48(12), 2101-2104
影响因子 2.5
文章链接 [url]http://www.sciencedirect.com/science?_ob=ArticleListURL&_method=list&_ArticleListID=779639059&_sort=d&view=c&_acct=C000054348&_version=1&_urlVersion=0&_userid=2012742&md5=ac8aca2b04c00dcf59f699114d343343[/url]
Abstract
P,N-ligands trans-4 and cis-5 with a cyclohexane backbone were easily synthesized. The key step was chiral resolution of (±)-trans-2-pyridylcyclohexanols with DBTA. Enantiopure trans isomer was subjected to Mitsunobu reaction and deprotection to give the corresponding cis isomer. These ligands have been successfully used in asymmetric hydrogenation of arylalkenes with up to 93% ee using 5 and 90% ee using 4 and asymmetric allylic alkylations with up to 95% ee using 5 and 93% ee using 4. Trans and cis P,N-ligands 4 and 5 all gave the product with the same configuration. It was suggested that the absolute configuration of the product was controlled by the configuration of the stereogenic pyridyl-bearing carbon of the ligands.
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