Synthesis and biological activities on batzelladine derivatives

被引:0
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作者
Shimokawa, Jun [1 ]
Iijima, Yumi
Hashimoto, Yuichi
Chiba, Harumi
Tanaka, Haruo
Nagasawa, Kazuo
机构
[1] Tokyo Univ Agr & Technol, Dept Biotechnol & Life Sci, Tokyo 1848588, Japan
[2] Univ Tokyo, Inst Mol & Cellular Biol, Tokyo 1130032, Japan
[3] Kitasato Univ, Sch Pharmaceut Sci, Tokyo 1088641, Japan
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
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.
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页码:145 / 150
页数:6
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