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Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides
Faculty
Pharmacy
Year:
2013
Type of Publication:
Article
Pages:
6886-6889
Authors:
Kothayer, Hend, Elshanawani, Abdalla A, Abu Kull, Mansour E, El-Sabbagh, Osama I, Shekhar, Malathy P. V, Brancale, Andrea, Jones, Arwyn T, Westwell, Andrew D
DOI:
10.1016/j.bmcl.2013.09.087
Journal:
BIOORGANIC \& MEDICINAL CHEMISTRY LETTERS PERGAMON-ELSEVIER SCIENCE LTD
Volume:
23
Research Area:
Pharmacology \& Pharmacy; Chemistry
ISSN
ISI:000327787700070
Keywords :
E2 ubiquitin conjugating enzyme, Rad6B, Triazines, Breast cancer, MDA-MB-231, MCF-7
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. (C) 2013 Elsevier Ltd. All rights reserved.
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