Synthesis of Novel Macrolactam and Macroketone Analogues of Migrastatin from D‐Glucal and Comparison with Macrolactone and Acyclic Analogues: A Dorrigocin A Congener Is a Potent Inhibitor of Gastric Cancer Cell Migration
摘要：
Novel macrolactam and macroketone analogues of the migrastatin macrolide core have been synthesised from tri- O -acetyl- D -glucal in order to facilitate structure-activity studies. The Horner olefination, followed by ring-closing metathesis were key steps in the synthesis of the macroketone. The ability of the macroketone and macrolactam derivatives to inhibit the migration of gastric tumour cells as determined using a transwell migration assay were compared with macrolactone analogues and dorrigocin A analogues. One dorrigocin A congener was the most potent inhibitor of gastric cancer cell migration.( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
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关键词：
Carbohydrates Tumour cell migration inhibitor Cancer Horner olefination Migrastatin Dorrigocin A Natural products
DOI：
10.1002/ejoc.200701192
被引量：
年份：
2010
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