81639-89-6

Upstream product

• 1443-80-7 4-cyanophenyl methyl ketone 
• 38868-10-9 triethyl phosphonoacetate anion 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 

Downstream Products

• 81639-96-5 4-(2-Cyano-1-methyl-cyclopropyl)-benzonitrile 
• 81639-94-3 2-(4-Methoxy-phenyl)-2-methyl-cyclopropanecarboxylic acid amide 
• 81639-92-1 2-(4-Cyano-phenyl)-2-methyl-cyclopropanecarboxylic acid amide 
• 81639-91-0 2-(4-Cyano-phenyl)-2-methyl-cyclopropanecarboxylic acid 

Relevant academic research and scientific papers

Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor

The histone acetyltransferases, CREB binding protein (CBP) and EP300, are master transcriptional co-regulators that have been implicated in numerous diseases, such as cancer, inflammatory disorders, and neurodegeneration. A novel, highly potent, orally bioavailable EP300/CBP histone acetyltransferase (HAT) inhibitor, CPI-1612 or 17, was developed from the lead compound 3. Replacement of the indole scaffold of 3 with the aminopyridine scaffold of 17 led to improvements in potency, solubility, and bioavailability. These characteristics resulted in a 20-fold lower efficacious dose for 17 relative to lead 3 in a JEKO-1 tumor mouse xenograft study.

COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS

Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.

P300/CBP HAT INHIBITORS AND METHODS FOR THEIR USE

Provided are compounds of Formula (I) : and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

Catalytic Asymmetric Transfer Hydrogenation of trans-Chalcone Derivatives Using BINOL-derived Boro-phosphates

Chiral phosphoric-acid-catalyzed asymmetric reductions of trans-chalcones have been investigated in this work. A BINOL-derived boro-phosphate-catalyzed asymmetric transfer hydrogenation of the carbon-carbon double bond of trans-chalcone derivatives employing borane as a hydride source was realized. This methodology provides a convenient procedure to access chiral dihydrochalone derivatives in high yields and with high enantioselectivities under mild conditions.

P300/CBP HAT INHIBITORS

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

The Photochemistry of 1-Cyano-2-methyl-3-phenylpropene and Ring substituted Derivatives

The E- and Z-isomers of 1-cyano-2-methyl-3-phenylpropene and ring-substituted derivatives of the E-isomer, are shown to fluoresce and undergo Z-E-isomerization and di-?-methane rearrangement on irradiation.The rate constants for these processes, obtained from fluorescence lifetimes and quantum yields, can be analysed in terms of an initial interaction between the two ? systems, facilitated by partial charge-transfer, followed by two diverging pathways, one, towards a diradicaloid species leading to cyclopropane formation, the other towards a 'zwitterionic' species and relaxation to the ground state and resulting in singlet state Z-E-isommerization.