期刊
TETRAHEDRON LETTERS
卷 55, 期 51, 页码 7015-7018出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2014.10.122
关键词
Triazines; Biguanides; Rad6B inhibitors; Antitumour agents
资金
- Higher Education Ministry of the Arab Republic of Egypt
- Algerian Consulate
Recently, we have identified the first inhibitors of Rad6B, an E2 enzyme essential for post-replication DNA repair and a potential new drug target for the treatment of breast cancer. We report two newly optimised synthetic routes to our [4-amino-6-(phenylamino)-1,3,5-triazin-2-yl]methyl 4-nitrobenzoate target compounds TZ8 and TZ9 with general applicability for further structure activity relationship studies around this pharmacophore. The key step involved the condensation/cyclisation between phenylbiguanide and either ethyl bromoacetate or dimethyloxalate in good yield. (C) 2014 Elsevier Ltd. All rights reserved.
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