Synthesis and biological activity of a fluorescent schweinfurthin analogue.
Synthesis and biological activity of a fluorescent schweinfurthin analogue.
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DOI：
10.1016/j.bmc.2009.04.071
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发表时间：
2009-07-01
影响因子：
3.5
通讯作者：
Wiemer DF
中科院分区：
文献类型：
--
作者：
Kuder CH;Neighbors JD;Hohl RJ;Wiemer DF
大多数天然schweinfurthins是有效的和选择性的细胞生长抑制剂，如国家癌症研究所的60细胞系筛选所测量的。由于这些天然产物的供应有限，我们已经启动了一项旨在合成它们的计划。迄今为止，这一努力已导致三个天然schweinfurthins和40多个类似物的制备，并对这些化合物的测定提供了一些了解在这个家庭的结构-活性关系。进一步开发schweinfurthins作为化疗药物将受益于其作用机制的表征。这种观点导致了荧光schweinfurthin类似物的开发，该类似物保留了天然产物的差异活性，但具有促进其在细胞内可视化的特性。合成了一种荧光schweinfurthin类似物，并对其生物活性和亚细胞定位进行了研究。
Most of the natural schweinfurthins are potent and selective inhibitors of cell growth as measured by the National Cancer Institute’s 60-cell line screen. Due to the limited supply of these natural products, we have initiated a program aimed at their synthesis. To date, this effort has led to the preparation of three natural schweinfurthins and more than 40 analogues, and assays on these compounds have afforded some understanding of structure-activity relationships in this family. Further development of schweinfurthins as chemotherapeutic agents would benefit from characterization of their mechanism(s) of action. This perspective led to development of a fluorescent schweinfurthin analogue that retains the differential activity of the natural products, and yet has properties that facilitate its visualization within cells. Synthesis of a fluorescent schweinfurthin analogue has been accomplished, and its biological activity and sub-cellular localization have been studied.
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影响因子：
64.8
作者：
SCHIFF, PB;FANT, J;HORWITZ, SB
通讯作者：
HORWITZ, SB
影响因子：
15
作者：
WANI, MC;TAYLOR, HL;MCPHAIL, AT
通讯作者：
MCPHAIL, AT
影响因子：
64.8
作者：
Uehata, M;Ishizaki, T;Narumiya, S
通讯作者：
Narumiya, S
DOI：
10.1080/10575630008043774
发表时间：
2000-01-01
期刊：
NATURAL PRODUCT LETTERS
影响因子：
--
作者：
Beutler, JA;Jato, J;Boyd, MR
通讯作者：
Boyd, MR
影响因子：
3.5
作者：
Neighbors, JD;Salnikova, MS;Wiemer, DF
通讯作者：
Wiemer, DF