title: Design, synthesis and biological evaluation of novel hydroxamic acids bearing artemisinin skeleton.
abstract: A series of novel hydroxamic acids bearing artemisinin skeleton was designed and synthesized. Some compounds in this series exhibited moderate inhibition against the whole cell HDAC enzymes. Especially, compound 6g displayed potent cytotoxicity against three human cancer cell lines, including HepG2 (liver cancer), MCF-7 (breast cancer) and HL-60 (leukemia cancer), with IC50 values of 2.50, 2.62 and 1.28μg/mL, respectively. Docking studies performed with two potent compounds 6a and 6g using Autodock Vina showed that both compounds bound to HDAC2 with relatively high binding affinities from -7.1 to 7.0kcal/mol compared to SAHA (-7.4kcal/mol). It was found in this research that most of the target compounds seemed to be more cytotoxic toward blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells.
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam.
authors.forename: Vu Thi
authors.initials: VT
authors.lastname: Ha
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam.
authors.forename: Vu Tuan
authors.initials: VT
authors.lastname: Kien
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam.
authors.forename: Le Huy
authors.initials: le H
authors.lastname: Binh
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam.
authors.forename: Vu Dinh
authors.initials: VD
authors.lastname: Tien
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam.
authors.forename: Nguyen Thi Thuy
authors.initials: NT
authors.lastname: My
authors.affiliation: Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, Viet Nam.
authors.forename: Nguyen Hai
authors.initials: NH
authors.lastname: Nam
authors.affiliation: Synthèse et Physicochimie de Molécules d'Intérêt Biologique, UMR 5068, Université Paul Sabatier, 118, route de Narbonne, 31062 Toulouse cedex 9, France.
authors.forename: Michael
authors.initials: M
authors.lastname: Baltas
authors.affiliation: Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
authors.forename: Hyunggu
authors.initials: H
authors.lastname: Hahn
authors.affiliation: Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
authors.forename: Byung Woo
authors.initials: BW
authors.lastname: Han
authors.affiliation: Institute of Biotechnology, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
authors.forename: Do Thi
authors.initials: do T
authors.lastname: Thao
authors.affiliation: School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dai Co Viet, Hanoi, Viet Nam. Electronic address: vu.trankhac@hust.edu.vn.
authors.forename: Tran Khac
authors.initials: TK
authors.lastname: Vu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D056945:Hep G2 Cells; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D061986:MCF-7 Cells; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D006877:Hydroxamic Acids; C031327:artemisinin
keywords: Artemisinin; Cytotoxicity; Endoperoxide; Histone deacetylase (HDAC) inhibitors; Hydroxamic acids