title: Antitumor activity of 9(R)-dihydrotaxane analogs.
abstract: A novel reduced taxane, 13-acetyl-9(R)-dihydrobaccatin III (1) has been isolated from Taxus canadensis. The selective C-13 deacetylation of this isolate has allowed for the preparation of a wide variety of 9(R)-dihydrotaxane analogs. In general, this series has shown greater stability and water solubility than the 9-carbonyl series while retaining antimicrotubule and tumor cell cytotoxicity activities relative to taxol. Placement of polar functionalities at the C-7 position results in loss of activity whereas alkylation or acylation of either C-7 or C-9 hydroxyl groups ameliorate the activity.
authors.affiliation: Abbott Laboratories, Abbott Park, Illinois 60064-3500, USA.
authors.forename: L L
authors.initials: LL
authors.lastname: Klein
authors.forename: L
authors.initials: L
authors.lastname: Li
authors.forename: C J
authors.initials: CJ
authors.lastname: Maring
authors.forename: C M
authors.initials: CM
authors.lastname: Yeung
authors.forename: S A
authors.initials: SA
authors.lastname: Thomas
authors.forename: D J
authors.initials: DJ
authors.lastname: Grampovnik
authors.forename: J J
authors.initials: JJ
authors.lastname: Plattner
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D017239:Paclitaxel