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

Abstract : 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.
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01114407
Contributor : Laurent Jonchère <>
Submitted on : Friday, December 18, 2015 - 3:14:39 PM
Last modification on : Thursday, March 5, 2020 - 4:57:29 PM
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Chinh Pham The, Tuyet Anh Dang Thi, Thi Phuong Hoang, Quoc Anh Ngo, Duy Tien Doan, et al.. Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (10), pp.2244-6. ⟨10.1016/j.bmcl.2014.03.091⟩. ⟨hal-01114407⟩

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