title: Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity.
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.
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Thi  Tuyet Anh
authors.initials: T
authors.lastname: Dang
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: The Chinh
authors.initials: TC
authors.lastname: Pham
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Quoc Anh
authors.initials: QA
authors.lastname: Ngo
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Thi  Thu Ha
authors.initials: T
authors.lastname: Vu
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Tien Dung
authors.initials: TD
authors.lastname: Nguyen
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Duy Tien
authors.initials: DT
authors.lastname: Doan
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Thi Cham
authors.initials: TC
authors.lastname: Ba
authors.affiliation: 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.
authors.forename: M
authors.initials: M
authors.lastname: Jean
authors.affiliation: 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.
authors.forename: P
authors.initials: P
authors.lastname: van de Weghe
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam. Electronic address: ngvtuyen@hotmail.com.
authors.forename: Van Tuyen
authors.initials: VT
authors.lastname: Nguyen
mesh_terms: D016923:Cell Death / Q000187:drug effects; D003603:Cytotoxins / Q000737:chemistry* / Q000633:toxicity*; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D056945:Hep G2 Cells; D006801:Humans; D009842:Oligopeptides / Q000737:chemistry* / Q000633:toxicity*; D013237:Stereoisomerism
chemical_list: D003603:Cytotoxins; D009842:Oligopeptides; C467070:hemiasterlin
keywords: Cytotoxicity; Hemiasterlin; Tripeptides; Unnatural hemiasterlin