| 17192004 |
Jiang X, Ao L, Zhou C, Yang L, Zhang Q, Li H, Sun L, Wu X, Bai H, Zhao Y: Design, synthesis, and biological evaluation of new territrem B analogues. Chem Biodivers. 2005 Apr;2(4):557-67.
Some 23 analogues of the potent acetylcholinesterase (AChE) inhibitor territrem B (1) were designed, synthesized, and tested for their biological activities. Some of the new synthetic derivatives exhibited IC50 values for AChE inhibition in the upper micromolar range. Molecular-modeling studies indicated that a planar conformation seems to be crucial for AChE inhibition. The two N-atoms of the piperazine moieties in 5o, 5p, and 5r might further enhance the inhibitory effects. The cytotoxicities of selected compounds against six human tumor cell lines were also determined. |
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