1233145-41-9Relevant academic research and scientific papers
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing
Chen, Bailing,Feru, Frederic,Feutrill, John,Gero, Thomas W.,Gray, Nathanael S.,Groendyke, Brian J.,Li, Bin,Li, Zhengnian,Powell, Chelsea E.,Scott, David A.,Szabo, Hilary
, (2020/08/07)
The protein kinase TNK2 (ACK1) is an emerging drug target for a variety of indications, in particular for cancer where it plays a key role transmitting cell survival, growth and proliferative signals via modification of multiple downstream effectors by unique tyrosine phosphorylation events. Scaffold morphing based on our previous TNK2 inhibitor XMD8-87 identified urea 17 from which we developed the potent and selective compound 32. A co-crystal structure was obtained showing 32 interacting primarily with the main chain atoms of an alanine residue of the hinge region. Additional H-bonds exist between the urea NHs and the Thr205 and Asp270 residues.
ANILINOPYRIMIDINES AS HAEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) INHIBITORS
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Paragraph 00260, (2018/06/21)
The invention relates to HPK1 inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: where A, R1, R2, R3, R4, R5, R6, R16, R17, X1, X2, X3, X4, m, and n are described herein.
