Migrastatin Analogs

Danishefsky et al. also prepared migrastatin analogs and investigated the structure-activity relationships (SAR) studies for chamber cell migration assay with human endothelial cells (HUVECs) [70,74]. Scheme 9 shows the synthesis of two analogs. The intermediate 73 was converted to azide 81 and bromide 84, which were respectively transformed to macrolactam 83 and macroketone 87 analogs lacking the glutarimide moiety. Among the analogs prepared, these two compounds in particular showed stronger activity than the parent compound 63.

Scheme 9 Synthesis of migrastatin analogs
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