Studies directed towards the refinement of the pancratistatin cytotoxic pharmacophore

Studies directed towards the refinement of the pancratistatin cytotoxic pharmacophore
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DOI:
10.1016/s0960-894x(00)00614-4
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发表时间:
2001-01-22
影响因子:
2.7
通讯作者:
Boyd, MR
Boyd, MR
中科院分区:
医学4区
文献类型:
--
作者:
McNulty, J;Mao, J;Boyd, MR

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合成了抗癌/抗病毒药物泛曲他汀的两个脱氧类似物,它们的功能与最小结构的药效团互补,并进行了抗癌筛选。其中一个类似物表现出对某些肿瘤细胞系的选择性抑制,但其效力明显低于天然产物。最小结构的药效团现在已经从8个可能的结构精炼到3个。(C)2001爱思唯尔科学有限公司。保留所有权利。
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. (C) 2001 Elsevier Science Ltd. All rights reserved.