[Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine].
OBJECTIVE
To make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects.


METHODS
The 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.


RESULTS
Six 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.


CONCLUSIONS
Novel alkaloid esters are worthy to be intensively studied.
Ye
Xian-rong
XR
Institute of Materia Medica Chinese Academy of Medical Science, Peking Union Medical College, Beijing 100050, China. xianrongye@imm.ac.cn
Wu
Ke-mei
KM
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000473:pathology; D003110:Colonic Neoplasms / Q000473:pathology; D006248:Harringtonines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077863:Homoharringtonine; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D008113:Liver Neoplasms / Q000473:pathology; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D006248:Harringtonines; C007562:drupacine; D000077863:Homoharringtonine