Synthesis of the Macrolactone of Migrastatin and Analogues with Potent Cell-Migration Inhibitory Activity
- DIAS, Luiz C.
- FINELLI, Fernanda G.
- CONEGERO, Leila S.
- KROGH, Renata
- ANDRICOPULO, Adriano D.
DOIAbstract
The synthesis of the macrolactone core of migrastatin 2, its potent anti-metastasis analogue 34, and ester derivatives 35 and 38 are reported. The approach involves the use of a dihydroxylation reaction to establish the desired C-8 stereocenter followed by a metathesis cyclization reaction. The effects of the compounds on the migration and invasion of human breast cancer cells were evaluated by using the wound-healing and the Boyden-chamber cell-migration and cell-invasion assays. The results revealed a high potency of the macrolactones 2 and 34 and the ester analogues 35 and 38, which suggests they have potential as antimetastatic agents.Fundo de Apoio ao Ensino e Pesquisa da UNICAMP (FAEP-UNICAMP)Fundo de Apoio ao Ensino e Pesquisa - UNIC...
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