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

…, K Chun, H Kim, HY Kim, JS Kang, JI Lee…

Index: Park, Chun-Ho; Lee, Chulho; Yang, Jee Sun; Joe, Bo-Young; Chun, Kwangwoo; Kim, Hyuntae; Kim, Hye Yun; Kang, Jong Soon; Lee, Jangik I.; Kim, Myung-Hwa; Han, Gyoonhee Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 12 p. 2655 - 2660

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Citation Number: 8

Abstract

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 ...