title: Synthesis and biological evaluation of 9α- and 9β-hydroxyamino-parthenolides as novel anticancer agents.
abstract: A series of 9α-hydroxyamino-parthenolides 3-10, 9β-hydroxyamino-parthenolides 11-13 and 9α-hydroxy-1β,10α-epoxyamino-parthenolides 15-19 were efficiently synthesized starting from 9α-hydroxyparthenolide 1 and 9β-hydroxyparthenolide 2, which were isolated from Anvillea radiata. Compounds 1-13 and 15-19 were evaluated for their in vitro anticancer activity by the MTT colorimetric assay against one murine and six human cancer cell lines. This work provides new details about the structural requisites for anticancer activity.
authors.affiliation: Laboratoire de Chimie Physique & de Chimie Bioorganique, URAC 22, Université Hassan II Mohammedia-Casablanca, BP 146, 28800 Mohammedia, Morocco.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Moumou
authors.affiliation: Laboratoire de Chimie Physique & de Chimie Bioorganique, URAC 22, Université Hassan II Mohammedia-Casablanca, BP 146, 28800 Mohammedia, Morocco; Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France.
authors.forename: Abderrahman
authors.initials: A
authors.lastname: El Bouakher
authors.affiliation: Laboratoire de Chimie Physique, équipe RICM UMR-ISP 1282, Faculté de Pharmacie, 31 Avenue Monge, 37200 Tours, France.
authors.forename: Hassan
authors.initials: H
authors.lastname: Allouchi
authors.affiliation: Laboratoire de Chimie Physique & de Chimie Bioorganique, URAC 22, Université Hassan II Mohammedia-Casablanca, BP 146, 28800 Mohammedia, Morocco.
authors.forename: Ahmed
authors.initials: A
authors.lastname: El Hakmaoui
authors.affiliation: Laboratoire de Chimie Biomoléculaires, Substances Naturelles et Réactivité, URAC16, Faculté des Sciences Semlalia, BP 2390, Bd My Abdellah, 40000 Marrakech, Morocco.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Benharref
authors.affiliation: Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, CP205/1, 1050 Brussels, Belgium.
authors.forename: Véronique
authors.initials: V
authors.lastname: Mathieu
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France. Electronic address: gerald.guillaumet@univ-orleans.fr.
authors.forename: Gérald
authors.initials: G
authors.lastname: Guillaumet
authors.affiliation: Laboratoire de Chimie Physique & de Chimie Bioorganique, URAC 22, Université Hassan II Mohammedia-Casablanca, BP 146, 28800 Mohammedia, Morocco. Electronic address: akssira@fstm.ac.ma.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Akssira
mesh_terms: D000588:Amines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D008968:Molecular Conformation; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D000970:Antineoplastic Agents; D012717:Sesquiterpenes; C002669:parthenolide
keywords: 9-Hydroxyamino-parthenolides; 9-Hydroxyparthenolides; 9α-Hydroxy-1β,10α-epoxyamino-parthenolides; 9α-Hydroxy-1β,10α-epoxyparthenolides; Anticancer activity