SYNTHESIS AND BIOLOGICAL ACTIVITIES ON BATZELLADINE DERIVATIVES

摘要

Structure-activity relationship studies on batzelladines A and D were examined.Seven batzelladine derivatives,including 24-epi-batzelladine A(3)and 7-epi-batzelladine D(4),were synthesized.The inhibitory activity of these derivatives on binding of gp120 with CD4 was evaluated by the use of ELISA-based assay method.For the potent biological activities of batzelladines,tricyclic guanidine moiety,a common structure of batzelladine A and D,and side chain bearing guanidine functional group were found to be mandatory.