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

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

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Park CH,Lee C,Yang JS,Joe BY,Chun K,Kim H,Kim HY,Kang JS,Lee JI,Kim MH,Han G

doi

10.1016/j.bmcl.2014.04.058

subject

Has Abstract

pub_date

2014-06-15 00:00:00

pages

2655-60

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00406-5

journal_volume

24

pub_type

杂志文章

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