title: Gamma-lactones alpha,beta- and beta,gamma-fused to carbocycles as novel antiproliferative drugs.
abstract: A set of gamma-lactones alpha,beta-fused and beta,gamma-fused to carbocycles have been synthesized and evaluated for their in vitro antiproliferative activities using the human cancer cell lines SW1573 (lung), T-47D (breast) and WiDr (colon). The compounds are obtained by intramolecular ring closing metathesis of the corresponding dienes. Active compounds exhibited GI(50) values in the range 8-18 microM. A structure-activity relationship is also discussed.
authors.affiliation: Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
authors.forename: Leticia G
authors.initials: LG
authors.lastname: León
authors.forename: Rubén P
authors.initials: RP
authors.lastname: Machín
authors.forename: Carmen M
authors.initials: CM
authors.lastname: Rodríguez
authors.forename: José L
authors.initials: JL
authors.lastname: Ravelo
authors.forename: Víctor S
authors.initials: VS
authors.lastname: Martín
authors.forename: José M
authors.initials: JM
authors.lastname: Padrón
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007783:Lactones