3-脱氧二氢石蒜碱的合成：结构最小的泛克他汀药效团的优化
A synthesis of 3-deoxydihydrolycoricidine: refinement of a structurally minimum pancratistatin pharmacophore.
作者信息
McNulty James, Larichev Vladimir, Pandey Siyaram
机构信息
Department of Chemistry, McMaster University, 1280 Main Street West, Hamilton, Ont., Canada L8S 4M1.
出版信息
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5315-8. doi: 10.1016/j.bmcl.2005.08.024. Epub 2005 Sep 23.
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.
本文描述了3-脱氧二氢石蒜碱的合成，该化合物是阐明水仙环素抗癌药效基团的关键要素。对该化合物的生物学评估表明，其对肿瘤细胞的活性明显低于水仙环素。除了先前确定的那些特征外，现在明确确定具有2,3,4-三醇官能化的C环是强效抗癌活性的最低药效基团要素。
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