111974-74-4, Name is 11-(1-Piperazinyl)-dibenzo[b,f][1,4]thiazepine dihydrochloride, molecular formula is C17H19Cl2N3S, HPLC of Formula: C17H19Cl2N3S, belongs to piperazines compound, is a common compound. In a patnet, author is Lee, Eun, once mentioned the new application about 111974-74-4.
Discovery of 5-Phenoxy-2-aminopyridine Derivatives as Potent and Selective Irreversible Inhibitors of Bruton’s Tyrosine Kinase
As a member of the tyrosine protein kinase Tec (TEC) family, Bruton’s tyrosine kinase (BTK) is considered a promising therapeutic target due to its crucial roles in the B cell receptor (BCR) signaling pathway. Although many types of BTK inhibitors have been reported, there is an unmet need to achieve selective BTK inhibitors to reduce side effects. To obtain BTK selectivity and efficacy, we designed a novel series of type II BTK inhibitors which can occupy the allosteric pocket induced by the DFG-out conformation and introduced an electrophilic warhead for targeting Cys481. In this article, we have described the structure-activity relationships (SARs) leading to a novel series of potent and selective piperazine and tetrahydroisoquinoline linked 5-phenoxy-2-aminopyridine irreversible inhibitors of BTK. Compound 18g showed good potency and selectivity, and its biological activity was evaluated in hematological tumor cell lines. The in vivo efficacy of 18g was also tested in a Raji xenograft mouse model, and it significantly reduced tumor size, with 46.8% inhibition compared with vehicle. Therefore, we have presented the novel, potent, and selective irreversible inhibitor 18g as a type II BTK inhibitor.
I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 111974-74-4 help many people in the next few years. HPLC of Formula: C17H19Cl2N3S.
Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics