title: Design and synthesis of antitumor compounds based on the cytotoxic diterpenoids from the genus Rabdosia.
abstract: Two active sites responsible for antitumor activity, an oxirane ring and an alpha-methylene-cyclopentanone moiety, have been extracted from studies on the structure-activity relationship of the cytotoxic diterpenoids isolated from Rabdosia shikokiana. Series of the simplified cyclopentanone derivatives containing both of the two active sites in the molecule have been synthesized and evaluated for cytotoxicity against P 388 cells. The compounds possessing both of two active sites displayed cytotoxicity at a concentration of 1 microgram/ml, while those possessing a single active site showed no activity.
authors.affiliation: Institute for Chemical Research, Kyoto University, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Fuji
authors.forename: H J
authors.initials: HJ
authors.lastname: Xu
authors.forename: H
authors.initials: H
authors.lastname: Tatsumi
authors.forename: H
authors.initials: H
authors.lastname: Imahori
authors.forename: N
authors.initials: N
authors.lastname: Ito
authors.forename: M
authors.initials: M
authors.lastname: Node
authors.forename: M
authors.initials: M
authors.lastname: Inaba
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis*; D004224:Diterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D010946:Plants, Medicinal / Q000032:analysis*; D014407:Tumor Cells, Cultured
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes