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Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity

Abstract : 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.
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01080910
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Submitted on : Friday, November 7, 2014 - 3:32:51 PM
Last modification on : Thursday, March 5, 2020 - 4:58:05 PM
Long-term archiving on: : Sunday, February 8, 2015 - 10:11:13 AM

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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 bioisosteric hemiasterlin analogues with extremely high cytotoxicity. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (22), pp.5216-5218. ⟨10.1016/j.bmcl.2014.09.065⟩. ⟨hal-01080910⟩

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