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新型环状姜黄素类似物的设计、合成及细胞生长抑制活性

Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues.

作者信息

Youssef Dani, Nichols Christie E, Cameron T Stanley, Balzarini Jan, De Clercq Erik, Jha Amitabh

机构信息

Département des Sciences, Université Sainte-Anne, Church Point, NS, Canada B0W 1M0.

出版信息

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5624-9. doi: 10.1016/j.bmcl.2007.07.079. Epub 2007 Aug 22.

Abstract

A series of novel cyclic analogues of curcumin were synthesized and analyzed for in vitro cytostatic activity. Condensation of 2-acetylcycloalkanones with a variety of aromatic aldehydes resulted in the formation of 2-arylidene-6-(3-arylacryoyl)-cycloalkanone derivatives. A number of these analogues were found to have significant anticancer activity against representative murine and human cancer cell lines during in vitro bioassays. This corroborated with in vitro cytostatic activity against a panel of 60 cell lines studied at the National Cancer Institute (USA).

摘要

合成了一系列新型姜黄素环状类似物,并对其体外细胞生长抑制活性进行了分析。2-乙酰基环烷酮与多种芳香醛缩合,生成了2-亚芳基-6-(3-芳基丙烯酰基)-环烷酮衍生物。在体外生物测定中,发现许多此类类似物对代表性的小鼠和人类癌细胞系具有显著的抗癌活性。这与在美国国立癌症研究所对一组60种细胞系进行的体外细胞生长抑制活性研究结果相佐证。

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