2. Academic Validation
  3. Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity

Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5216-8. doi: 10.1016/j.bmcl.2014.09.065.
Thi Tuyet Anh Dang 1,  The Chinh Pham 1,  Quoc Anh Ngo 1,  Thi Thu Ha Vu 1,  Tien Dung Nguyen 1,  Duy Tien Doan 1,  Thi Cham Ba 1,  M Jean 2,  P van de Weghe 3,  Van Tuyen Nguyen 4
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 Biologiques, 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 Biologiques, 2, Avenue du Prof L. Bernard, F-35043 Rennes Cedex, France. Electronic address: pierre.van-de-weghe@univ-rennes1.fr.
  • 4 Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam. Electronic address: ngvtuyen@hotmail.com.
PMID: 25442315 DOI: 10.1016/j.bmcl.2014.09.065
Abstract

In this Letter, the synthesis and the evaluation of the cytotoxicity of new hemiasterlin analogues were reported. The indole moiety was replaced respectively by benzofurane, naphthalene and 4-bromobenzene groups. Most of these derivatives possess strong cytotoxic activity on two human tumour cell lines (KB and Hep-G2), and some analogues showed comparable cytotoxic activity to that observed for paclitaxel and ellipticine, against KB and Hep-G2 Cancer cell lines.

Keywords

Cytotoxicity; Hemiasterlin; Tripeptides; Unnatural hemiasterlin.

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