5593-28-2

Upstream product

• 122-01-0 4-chloro-benzoyl chloride 
• 109-77-3 malononitrile 

Downstream Products

• 90845-30-0 2-(p-chlorobenzoyl)-2-cyanoketenimine 
• 5354-43-8 3-Amino-3-chlor-2-<4-chlor-benzoyl>-acrylonitril 
• 5515-14-0 2-((4-chlorophenyl)(methoxy)methylene)malononitrile 
• 1354825-95-8 C₂₂H₂₂ClN₅O₂ 
• 1354825-96-9 C₂₃H₂₃ClN₆O₂ 
• 1354825-97-0 BrH*C₁₅H₁₇ClN₆ 
• 42754-62-1 5-Amino-3-(4-chlorophenyl)-1H-pyrazole-4-carbonitrile 
• 42754-70-1 4-Amino-3-(4-chlorophenyl)pyrazolo<3,4-d>pyrimidine 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of proteolysis targeting chimeras (PRoTACS) for the dual degradation of IGF-1R and SrC

A focused PROTAC library was developed to degrade both IGF-1R and Src proteins, which are associated with various cancers. PROTACs with IGF-1R and Src degradation potentials were synthesized by tethering different inhibitor warhead units and the E3 ligase (CRBN) recruiting-pomalidomide with various linkers. The designed PROTACs 12a–b inhibited the proliferation and migration of MCF7 and A549 cancer cells with low micromolar potency (1–5 μM) in various cellular assays.

HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF

Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.

Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors

Fyn is a member of the Src-family of nonreceptor protein-tyrosine kinases. Its abnormal activity has been shown to be related to various human cancers as well as to severe pathologies, such as Alzheimer's and Parkinson's diseases. Herein, a structure-based drug design protocol was employed aimed at identifying novel Fyn inhibitors. Two hits from commercial sources (1, 2) were found active against Fyn with Ki of about 2 μM, while derivative 4a, derived from our internal library, showed a Ki of 0.9 μM. A hit-to-lead optimization effort was then initiated on derivative 4a to improve its potency. Slightly modifications rapidly determine an increase in the binding affinity, with the best inhibitors 4c and 4d having Kis of 70 and 95 nM, respectively. Both compounds were found able to inhibit the phosphorylation of the protein Tau in an Alzheimer's model cell line and showed antiproliferative activities against different cancer cell lines. (Chemical Equation Presented).

PROTEIN KINASE INHIBITORS AND METHODS OF TREATMENT

The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.