Synthesis of [1,2]oxazolo[5,4-e]indazoles as antitumour agents
Synthesis of [1,2]oxazolo[5,4-e]indazoles as antitumour agents
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DOI：
10.1016/j.tet.2013.05.083
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发表时间：
2013-08-05
期刊：
影响因子：
2.1
通讯作者：
Cirrincione, Girolamo
中科院分区：
文献类型：
--
作者：
Barraja, Paola;Spano, Virginia;Cirrincione, Girolamo
用一种通用、方便的方法制备了一系列[1,2]恶唑[5,4-e]吲哚环体系的40个衍生物，产率较高。茚唑-4-酮体系上的[1,2]恶唑环通过相应的烯酰胺酮与盐酸羟胺的反应而被合成。Bethesda国家癌症研究所对标题环体系的衍生物进行了测试，其中一种（13t）在低微摩尔浓度下对所有54种人类肿瘤细胞系都显示出生长抑制活性。(C) 2013 Elsevier Ltd.版权所有。
A series of 40 derivatives of the [1,2]oxazolo[5,4-e]indazoles ring system have been prepared with good yields using a versatile and convenient route. Annelation of the [1,2]oxazole ring on the indazole-4-one system was achieved by reaction of the corresponding enaminoketones with hydroxylamine hydrochloride. Derivatives of the title ring system were tested by the National Cancer Institute of Bethesda and one of them (13t) showed growth-inhibitor activity against all the 54 human tumour cell lines generally at low micromolar concentrations. (C) 2013 Elsevier Ltd. All rights reserved.