RESUMO
<p><b>AIM</b>To design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C3'-N of taxol side chain.</p><p><b>METHODS</b>Protective 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.</p><p><b>RESULTS</b>The seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C3'-N.</p><p><b>CONCLUSION</b>It might provide some rational basis for further structral modification.</p>
Assuntos
Humanos , Antineoplásicos Fitogênicos , Química , Farmacologia , Linhagem Celular Tumoral , Neoplasias do Colo , Patologia , Ésteres , Harringtoninas , Química , Farmacologia , Células KB , Neoplasias Hepáticas , Patologia , Estrutura MolecularRESUMO
<p><b>AIM</b>To provide basic data for the synthesis of new sinomenine derivatives.</p><p><b>METHODS</b>The C ring in sinomenine was modified.</p><p><b>RESULTS</b>Seven compounds were prepared and screened for anti-inflammatory and analgesic activities. Compounds 2 and 5 showed better activities.</p><p><b>CONCLUSION</b>Modification of the C ring in sinomenine should be worthy to be studied further.</p>
Assuntos
Animais , Camundongos , Ratos , Anti-Inflamatórios não Esteroides , Farmacologia , Edema , Patologia , Conformação Molecular , Estrutura Molecular , Morfinanos , Farmacologia , Medição da Dor , Plantas Medicinais , Química , Sinomenium , QuímicaRESUMO
<p><b>AIM</b>To make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>Novel alkaloid esters are worthy to be intensively studied.</p>