Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity
Résumé
In this article, we report a convenient and efficient method for the synthesis of new simplified derivatives
of hemiasterlin in which the α,α-dimethylbenzylic moiety A is replaced by α,β-unsaturated aryl groups
as Michael acceptor. Most of these derivatives have a strong cytotoxic activity on three human tumor
cell lines (KB, Hep-G2 and MCF7). Analogs 17b and 17f showed a high cytotoxicity against KB and
Hep-G2 cancer cell lines comparable to paclitaxel and ellipticine.
Domaines
Chimie thérapeutique
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