Discovery and optimization of cyclohexane-1,4-diamines as allosteric MALT1 inhibitors
Abstract
Inhibition of mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) is a promising strategy to modulate NF-κB signaling, with the potential to treat B-cell lymphoma and autoimmune diseases. We describe the discovery and optimization of (1s,4s)-N,N'-diaryl cyclohexane-1,4-diamines, a novel series of allosteric MALT1 inhibitors, resulting in compound 8 with single digit micromolar cell potency. X-ray analysis confirms that...
Paper Details
Title
Discovery and optimization of cyclohexane-1,4-diamines as allosteric MALT1 inhibitors
Published Date
Jan 1, 2022
Volume
227
Pages
113925 - 113925
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