Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111590
Abstract: Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested… read more here.
Keywords: piperazinyl aminopyrimidine; aminopyrimidine derivatives; jak2 flt3; flt3 ... See more keywords
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00091
Abstract: A series of 2-aminopyrimidine derivatives were designed and synthesized as highly selective FGFR4 inhibitors. One of the most promising compounds 2n tightly bound FGFR4 with a Kd value of 3.3 nM and potently inhibited its… read more here.
Keywords: new selective; aminopyrimidine derivatives; fgfr4 inhibitors; derivatives new ... See more keywords
Synthesis of 2-Aminopyrimidine Derivatives and Their Evaluation as β-Glucuronidase Inhibitors: In Vitro and In Silico Studies
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27227786
Abstract: Currently the discovery and development of potent β-glucuronidase inhibitors is an active area of research due to the observation that increased activity of this enzyme is associated with many pathological conditions, such as colon cancer,… read more here.
Keywords: aminopyrimidine derivatives; derivatives evaluation; glucuronidase inhibitors; evaluation glucuronidase ... See more keywords