title: Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety.
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.
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Chinh Pham
authors.initials: CP
authors.lastname: The
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Tuyet Anh Dang
authors.initials: TA
authors.lastname: Thi
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Thi Phuong
authors.initials: TP
authors.lastname: Hoang
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: 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: Thu Ha Nguyen
authors.initials: TH
authors.lastname: Thi
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Tham Pham
authors.initials: TP
authors.lastname: Thi
authors.affiliation: Institute of Chemistry-Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Thu Ha Vu
authors.initials: TH
authors.lastname: Thi
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 Biologique, 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 Biologique, 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.
authors.forename: Tuyen Nguyen
authors.initials: TN
authors.lastname: Van
mesh_terms: D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D007624:KB Cells; D061986:MCF-7 Cells; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D009842:Oligopeptides; C467070:hemiasterlin
keywords: Cytotoxicity; Hemiasterlin; Tripeptides