Synthesis of new simplified hemiasterlin derivatives with 伪,尾-unsaturated carbonyl moiety

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• 作者：Chinh Pham The^a ; Tuyet Anh Dang Thi^a ; Thi Phuong Hoang^a ; Quoc Anh Ngo^a ; Duy Tien Doan^a ; Thu Ha Nguyen Thi^a ; Tham Pham Thi^a ; Thu Ha Vu Thi^a ; M. Jean^b ; P. van de Weghe^b ; ^{pierre.van-de-weghe@univ-rennes1.fr" class="auth_mail} ; Tuyen Nguyen Van^a ;
• 关键词：Hemiasterlin ; Cytotoxicity ; Tripeptides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 May 2014
• 年：2014
• 卷：24
• 期：10
• 页码：2244-2246
• 全文大小：528 K

文摘

In this Letter, we report a convenient and efficient method for the synthesis of new simplified derivatives of hemiasterlin in which the 伪,伪-dimethylbenzylic moiety A is replaced by 伪,尾-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.