期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 24, 页码 6886-6889出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.09.087
关键词
E2 ubiquitin conjugating enzyme; Rad6B; Triazines; Breast cancer; MDA-MB-231; MCF-7
资金
- Higher Education Ministry of the Arab Republic of Egypt
Series of substituted 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides have been synthesised, based on molecular modelling of candidate structures related to the previously reported Rad6B-inhibitory diamino-triazinylmethyl benzoate anticancer agents TZ8 and TZ9. Synthesis of the target compounds was readily accomplished in two steps from aryl biguanides via reaction of phenylhydrazine or benzylamines with key 4-amino-6-(arylamino)-1,3,5-triazine-2-carboxylate intermediates. These new triazine derivatives were tested for in vitro anticancer activity against the Rad6B expressing human breast cancer cell lines MDA-MB-231 and MCF-7. Active compounds, such as the triazinyl-carbohydrazides 3a-e, were found to exhibit low micromolar IC50 values particularly in the Rad6B-overexpressing MDA-MB-231 cell line. (C) 2013 Elsevier Ltd. All rights reserved.
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