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Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety

In this Letter, 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 h...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (10), p.2244-2246
Main Authors: The, Chinh Pham, Thi, Tuyet Anh Dang, Hoang, Thi Phuong, Ngo, Quoc Anh, Doan, Duy Tien, Thi, Thu Ha Nguyen, Thi, Tham Pham, Thi, Thu Ha Vu, Jean, M., van de Weghe, P., Van, Tuyen Nguyen
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Language:English
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Summary:In this Letter, 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.03.091