Design and Synthesis of Novel 3‐(2‐Aminopyridin‐3‐yl)‐1,2,4‐Triazolo[4,3‐b]Pyridazine Derivatives as a Reversible Bruton's Tyrosine Kinase Inhibitors

[摘要] Bruton's tyrosine kinase, a non‐receptor TEC family kinase, plays key role in B cell differentiation, proliferation, and survival. B cell receptor regulates the B cell's fate and cytokine release of B‐lineage lymphoid leukemia cells which are deeply related with the pathogenesis of B‐cell lineage of lymphoma and leukemia and autoimmune diseases. Thus, BTK protein regulation emerged as a promising therapeutic target for both various cancers and autoimmune diseases. Herein, we report the discovery of aminopyridin‐1,2,4‐triazolopyridazine derivatives as a reversible BTK inhibitor, and in vitro enzyme assay and cell based assay result were reported.

[学科分类] 化学（综合）

[关键词] Reversible Bruton's kinase;BTK inhibitor;Triazolopyridazine derivative;Anticancer agent