Document Report Card

ID: ALA1128309

Journal: J Med Chem

Title: Antitumor activity of 9(R)-dihydrotaxane analogs.

Authors: Klein LL, Li L, Maring CJ, Yeung CM, Thomas SA, Grampovnik DJ, Plattner JJ.

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.

CiteXplore: 7739007

DOI: 10.1021/jm00009a009