针对泛癌抑素细胞毒性药效团优化的研究。
Studies directed towards the refinement of the pancratistatin cytotoxic pharmacophore.
作者信息
McNulty J, Mao J, Gibe R, Mo R, Wolf S, Pettit G R, Herald D L, Boyd M R
机构信息
Institute of Molecular Catalysis, Department of Chemistry, Brock University, St. Catharines, Ontario, Canada.
出版信息
Bioorg Med Chem Lett. 2001 Jan 22;11(2):169-72. doi: 10.1016/s0960-894x(00)00614-4.
Two deoxy-analogues of the anticancer/antiviral agent pancratistatin containing functionality complementary to the minimum structural pharmacophore were synthesized and subjected to anticancer screening. One of the analogues exhibited selective inhibition of certain tumor cell lines but was significantly less potent than the natural products. The minimum structural pharmacophore has now been refined from eight to three possible structures.
合成了两种抗癌/抗病毒药物棒丝氨酸内酯的脱氧类似物，它们具有与最小结构药效基团互补的功能，并进行了抗癌筛选。其中一种类似物对某些肿瘤细胞系表现出选择性抑制作用，但效力明显低于天然产物。现在，最小结构药效基团已从八种可能的结构优化为三种。
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