Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine.
- Author:
Xian-rong YE
1
;
Ke-mei WU
Author Information
- Publication Type:Journal Article
- MeSH: Antineoplastic Agents, Phytogenic; chemical synthesis; chemistry; pharmacology; Carcinoma, Hepatocellular; pathology; Colonic Neoplasms; pathology; Harringtonines; chemical synthesis; chemistry; pharmacology; Humans; KB Cells; drug effects; Liver Neoplasms; pathology; Tumor Cells, Cultured
- From: Acta Pharmaceutica Sinica 2003;38(12):919-923
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects.
METHODSThe C3 hydroxy groups of the cephlotaxine and drupacine were acylated by taxol side chain and its isomers to give a series of derivatives of cephlotaxine and drupacine.
RESULTSSix novel alkaloid esters were designed and synthesized. The pharmacological screening results showed that VIIIa, VIIIb, IXa and IXc exhibited significant activities on KB, HCT and Bel in vitro.
CONCLUSIONNovel alkaloid esters are worthy to be intensively studied.
