1142408-69-2Relevant academic research and scientific papers
Rational design, synthesis and biological profiling of new KDM4C inhibitors
Letfus, Vatroslav,Jeli?, Dubravko,Bokuli?, Ana,Petrini? Grba, Adriana,Ko?trun, Sanja
, (2019/12/09)
The human histone demethylases of the KDM4 family have been related to diseases such as prostate and breast cancer. Majority of currently known inhibitors suffer from the low permeability and low selectivity between the enzyme isoforms. In this study, toxoflavin motif was used to design and synthesize new KDM4C inhibitors with improved biological activity and in vitro ADME properties. Inhibitors displayed good passive cellular permeability and metabolic stability. However, diminishing of redox liability and consequently non-specific influence on cell viability still remains a challenge.
The facile synthesis of 6-azapurines by transformation of toxoflavins (7-azapteridines)
Nagamatsu, Tomohisa,Ma, Jun,Yoneda, Fumio
body text, p. 849 - 854 (2010/10/03)
This paper describes a reliable and facile synthesis of 6-azapurines (1,5-dimethyl-1H imidazo[4,5-e][1,2,4]triazin-6(5H)-ones) by treatment of toxoflavins (7-azapteridines) with 10% aqueous sodium hydroxide at 5-25 °C along with a benzilic acid type rearr
