Synthesis and antiproliferativeactivity of new vinca alkaloids containing an α,β-unsaturated aromatic side chain

  • Bioorg Med Chem Lett. 2015 Dec 1;25(23):5597-600. doi: 10.1016/j.bmcl.2015.10.040.
Quoc Anh Ngo  1 ,  Le Anh Nguyen  2 ,  Ngoc Binh Vo  2 ,  Thuy Hang Nguyen  2 ,  Fanny Roussi  3 ,  The Hung Nguyen  4 ,  Van Tuyen Nguyen  2
Affiliations
  • 1. Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, CauGiay, Hanoi, Viet Nam. Electronic address: [email protected].
  • 2. Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, CauGiay, Hanoi, Viet Nam.
  • 3. Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Université Paris Sud, 1 avenue de la terrasse, 91198 Gif sur Yvette Cedex, France.
  • 4. Ministry of Science and Technology, Viet Nam.
PMID: 26522953 DOI: 10.1016/j.bmcl.2015.10.040
Abstract

A new series of vinca-alkaloids derivatives containing various α,β-unsaturated aromatic side chains was synthesized. Four new vinca-alkaloids derivatives showed selective cytotoxicities against KB tumor cell lines with IC50 value below 0.1 μM, thus comparable with vinblastine.

Keywords
Cytotoxicity; Sarcodictyins; Tubulin; Vinca alkaloids.