A synthesis of 3-deoxydihydrolycoricidine: Refinement of a structurally minimum pancratistatin pharmacophore

被引:64
作者
McNulty, J
Larichev, V
Pandey, S
机构
[1] McMaster Univ, Dept Chem, Hamilton, ON L8S 4M1, Canada
[2] Univ Windsor, Dept Chem & Biochem, Windsor, ON N9B 3P4, Canada
关键词
D O I
10.1016/j.bmcl.2005.08.024
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of 3-deoxydihydrolycoricidine, a key element toward elucidation of the pancratistatin anticancer pharmacophore, is described. Biological evaluation of this compound showed it to be significantly less active against tumor cells than pancratistatin. In addition to those features previously identified, the requirement of a 2,3,4-triol functionalized ring-C is now definitely established as the minimum pharmacophoric element for potent anticancer activity. (c) 2005 Elsevier Ltd. All rights reserved.
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页码:5315 / 5318
页数:4
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