spc-839 has been researched along with thienopyrimidine* in 1 studies
1 other study(ies) available for spc-839 and thienopyrimidine
Article | Year |
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Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.
Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting analogues had good inhibitory activity against both nitric oxide and TNF-α, which are well-known inflammatory responses generated by activated NF-κB. However, no inhibitory activity against IKKβ was observed with these compounds. The thienopyrimidine-based analogues were subsequently screened for a target kinase, and FLT3, which is a potential target for acute myeloid leukemia (AML), was identified. Thienopyrimidine-based FLT3 inhibitors showed good inhibition profiles against FLT3 under 1μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML. Topics: Enzyme Activation; fms-Like Tyrosine Kinase 3; Humans; I-kappa B Kinase; Maleimides; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Quinazolines; Small Molecule Libraries | 2014 |