100281-35-4

Upstream product

• 5031-78-7 4-phenoxyacetophenone 
• 95-92-1 oxalic acid diethyl ester 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 108-95-2 phenol 

Relevant academic research and scientific papers

Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor

The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model.

Rationally Designed Polypharmacology: α-Helix Mimetics as Dual Inhibitors of the Oncoproteins Mcl-1 and HDM2

Protein–protein interactions (PPIs), many of which are dominated by α-helical recognition domains, play key roles in many essential cellular processes, and the dysregulation of these interactions can cause detrimental effects. For instance, aberrant PPIs involving the Bcl-2 protein family can lead to several diseases including cancer, neurodegenerative diseases, and diabetes. Interactions between Bcl-2 pro-life proteins, such as Mcl-1, and pro-death proteins, such as Bim, regulate the intrinsic pathway of apoptosis. p53, a tumor-suppressor protein, also has a pivotal role in apoptosis and is negatively regulated by its E3 ubiquitin ligase HDM2. Both Mcl-1 and HDM2 are upregulated in numerous cancers, and, interestingly, there is crosstalk between both protein pathways. Recently, synergy has been observed between Mcl-1 and HDM2 inhibitors. Towards the development of new anticancer drugs, we herein describe a polypharmacology approach for the dual inhibition of Mcl-1 and HDM2 by employing three densely functionalized isoxazoles, pyrazoles, and thiazoles as mimetics of key α-helical domains of their partner proteins.

Substituted pyrazole-containing compound, preparation method and applications thereof

The present invention provides a substituted pyrazole-containing compound, a preparation method and applications thereof, wherein the compound or a pharmaceutically acceptable salt thereof has a structure represented by a formula X defined in the specific

BTK INHIBITOR

Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).

Studies on hypolipidemic agents. II. 3-(4-phenoxybenzoyl)propionic acid derivatives

3-(4-Phenoxybenzoyl)propionic acids were prepared and tested for hypolipidemic activity in normal rats. A structure-activity relationship study showed that the 2-acetylthio derivative had hypolipidemic activity. Among these compounds, 2-acetylthio-[3-(4-c