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Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides

Kothayer, Hend, Elshanawani, Abdalla A., Abu Kull, Mansour E., El-Sabbagh, Osama I., Shekhar, Malathy P. V., Brancale, Andrea, Jones, Arwyn Tomos and Westwell, Andrew D. 2013. Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides. Biorganic and Medicinal Chemistry Letters 23 (24) , pp. 6886-6889. 10.1016/j.bmcl.2013.09.087

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Abstract

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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords: E2 ubiquitin conjugating enzyme; Rad6B; Triazines; Breast cancer; MDA-MB-231; MCF-7
Publisher: Elsevier
ISSN: 0960-894X
Last Modified: 17 Nov 2017 19:55
URI: http://orca.cf.ac.uk/id/eprint/56812

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