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Total synthesis and antiproliferative activity screening of (±)-aplicyanins A, B and E and related analogs
Sísa, Miroslav; Pla Queral, Daniel; Altuna, Marta; Francesch, Andrés; Cuevas, Carmen; Albericio Palomera, Fernando; Álvarez Domingo, Mercedes
Universitat de Barcelona
The first total synthesis of the indole alkaloids ()-aplicyanins A, B and E, plus seventeen analogs, all in racemic form is reported. Modifications to the parent compound included changing the number of bromine substituents on the indole, the groups on the indole nitrogen (H, Me or OMe), and/or the oxidation level of the heterocyclic core tetrahydropyrimidine. Each compound was screened against three human tumor cell lines, and fourteen of the newly synthesized compounds showed considerable cytotoxicity. The assay results were used to establish structure-activity relationships. These results suggest that the acetyl group moiety on the imine nitrogen, and the bromine at position 5 of the indole, are both critical to activity.
Medicaments antineoplàstics
Síntesi de fàrmacs
Alcaloides
Metabòlits marins
Antineoplastic agents
Drug synthesis
Alkaloids
Marine metabolites
(c) American Chemical Society , 2009
Artículo
info:eu-repo/semantics/acceptedVersion
American Chemical Society
         

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