Studies on the synthesis and antitumor activity of the derivatives of cephalotaxine alkaloid esters.
- Author:
Xian-rong YE
1
;
Yong-hai CHAI
;
Xing-nan LI
;
Ke-mei WU
Author Information
- Publication Type:Journal Article
- MeSH: Antineoplastic Agents, Phytogenic; chemical synthesis; chemistry; pharmacology; Cell Line, Tumor; Colonic Neoplasms; pathology; Esters; Harringtonines; chemical synthesis; chemistry; pharmacology; Humans; KB Cells; Liver Neoplasms; pathology; Molecular Structure
- From: Acta Pharmaceutica Sinica 2004;39(6):429-433
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C3'-N of taxol side chain.
METHODSProtective side chain acid VI (4'S,5'R) was prepared from optically active (2'R,3'S) methyl beta-phenyl glycidate I in five steps. The desired acids were coupled with cephlotaxine and drupacine respectively in the presence of 2-DPC/DMAP, followed by acidic hydrolysis and acylating to give novel alkloid esters with different substitutes on C3'-N.
RESULTSThe seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C3'-N.
CONCLUSIONIt might provide some rational basis for further structral modification.
