Studies on the synthesis and antitumor activity of the derivatives of cephalotaxine alkaloid esters

AimTo design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C_3′-N of taxol side chain． MethodsProtective side chain acid VI (4′S，5′R) was prepared from optically active (2′R，3′S) methyl β-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 C_3′-N． Results The seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C_3′-N． ConclusionIt might provide some rational basis for further structral modification．