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  • Title: [Studies on the synthesis and antitumor activity of the derivatives of cephalotaxine alkaloid esters].
    Author: Ye XR, Chai YH, Li XN, Wu KM.
    Journal: Yao Xue Xue Bao; 2004 Jun; 39(6):429-33. PubMed ID: 15491099.
    Abstract:
    AIM: To design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C3'-N of taxol side chain. METHODS: 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. RESULTS: The seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C3'-N. CONCLUSION: It might provide some rational basis for further structral modification.
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