99056-81-2Relevant articles and documents
Optimised synthesis of diamino-triazinylmethyl benzoates as inhibitors of Rad6B ubiquitin conjugating enzyme
Kothayer, Hend,Morelli, Matteo,Brahemi, Ghali,Elshanawani, Abdalla A.,Abu Kull, Mansour E.,El-Sabbagh, Osama I.,Shekhar, Malathy P.V.,Westwell, Andrew D.
, p. 7015 - 7018 (2014)
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.