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

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

  • Bioorg Med Chem Lett. 2014 May 15;24(10):2244-6. doi: 10.1016/j.bmcl.2014.03.091.
Chinh Pham The 1,  Tuyet Anh Dang Thi 1,  Thi Phuong Hoang 1,  Quoc Anh Ngo 1,  Duy Tien Doan 1,  Thu Ha Nguyen Thi 1,  Tham Pham Thi 1,  Thu Ha Vu Thi 1,  M Jean 2,  P van de Weghe 3,  Tuyen Nguyen Van 1
Affiliations

Affiliations

  • 1 Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
  • 2 Equipe Produits Naturels, Synthèses et Chimie Médicinale (PNSCM), UMR CNRS 6226-Institut des Sciences Chimiques de Rennes, Université de Rennes 1, UFR Sciences Pharmaceutiques et Biologique, 2, Avenue du Prof L. Bernard, F-35043 Rennes Cedex, France.
  • 3 Equipe Produits Naturels, Synthèses et Chimie Médicinale (PNSCM), UMR CNRS 6226-Institut des Sciences Chimiques de Rennes, Université de Rennes 1, UFR Sciences Pharmaceutiques et Biologique, 2, Avenue du Prof L. Bernard, F-35043 Rennes Cedex, France. Electronic address: pierre.van-de-weghe@univ-rennes1.fr.
PMID: 24745968 DOI: 10.1016/j.bmcl.2014.03.091
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.

Keywords

Cytotoxicity; Hemiasterlin; Tripeptides.

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