Synthesis and in vitro anticancer evaluation of some 4,6-diamino-1,3,5-triazine-2-carbohydrazides as Rad6 ubiquitin conjugating enzyme inhibitors
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文摘

Novel 4-amino-6-(arylamino)-1,3,5-triazine-2-carbohydrazides (3ae) and N′-phenyl-4,6-bis(arylamino)-1,3,5-triazine-2-carbohydrazides (6ae) have been synthesized.

To evaluate the efficacy of newly synthesized triazines in Rad6 inhibitory activities, in vitro ubiquitin conjugation assays were performed in comparison with our previously reported Rad6 inhibitor TZ9 as well as their in vitro anticancer activity against several human cancer cell lines.

Our new triazines showed better Rad6B inhibitory activities and anticancer properties compared to previously reported Rad6B inhibitor TZ9 in in vitro evaluations.

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