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吡喃环上带有硝基或氨基取代侧链的新型吡喃呫吨酮的设计与合成。评估它们对乳腺癌细胞的生长抑制活性。

Design and synthesis of new pyranoxanthenones bearing a nitro group or an aminosubstituted side chain on the pyran ring. Evaluation of their growth inhibitory activity in breast cancer cells.

作者信息

Kolokythas George, Kostakis Ioannis K, Pouli Nicole, Marakos Panagiotis, Kousidou Olga Ch, Tzanakakis George N, Karamanos Nikos K

机构信息

Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece.

出版信息

Eur J Med Chem. 2007 Mar;42(3):307-19. doi: 10.1016/j.ejmech.2006.10.018. Epub 2006 Dec 4.

Abstract

Some new 2,6-disubstituted pyrano- and 1,2-dihydropyrano[2,3-c]xanthen-7-ones have been synthesized and their antiproliferative activity has been evaluated against MDA-MB-231 breast cancer cells. The antiproliferative activity evaluation of the compounds provided evidence that a dimethylamino substituted side chain and the presence of 1,2 double bond play a key role in cell growth inhibition. Among the tested derivatives the 6-dimethylaminoethylamino-2-nitropyranoxanthenone analogue possessed a significant inhibitory effect in a wide range of concentrations.

摘要

一些新型的2,6-二取代吡喃并[2,3-c]呫吨-7-酮和1,2-二氢吡喃并[2,3-c]呫吨-7-酮已被合成,并对其针对MDA-MB-231乳腺癌细胞的抗增殖活性进行了评估。化合物的抗增殖活性评估表明,二甲基氨基取代的侧链和1,2-双键的存在在细胞生长抑制中起关键作用。在所测试的衍生物中,6-二甲基氨基乙氨基-2-硝基吡喃呫吨酮类似物在广泛的浓度范围内具有显著的抑制作用。

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