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Title 

Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors

Authors 

C H ParkC LeeJ S YangB Y JoeK ChunH KimH Y KimJong Soon KangJ I LeeM H KimG Han

Publisher 

Elsevier

Issue Date 

2014

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 12, pp. 2655-2660

Keywords 

Acute myeloid leukemia (AML)Anti-inflammationFLT3IKKβThienopyrimidine

Abstract 

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 1 μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2014.04.058

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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