51919-89-2

Upstream product

• 2840-28-0 3-amino-4-chloro-benzoic acid 
• 506-59-2 N,N-dimethylammonium chloride 
• 2486-71-7 4-amino-3-chlorobenzoic acid 
• 38818-50-7 4-chloro-3-nitro-benzoyl chloride 
• 5334-04-3 4-chloro-3-nitro-benzoic acid dimethylamide 

Downstream Products

• 1189813-84-0 methyl 2-(2-chloro-5-(dimethylcarbamoyl)phenylcarbamoyl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-8-carboxylate 
• 1365345-71-6 C₂₃H₂₀BrClN₂O₃S 
• 1386979-56-1 2-methoxy-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid (2-chloro-5-dimethylcarbamoyl-phenyl)-amide 
• 1346161-50-9 8-bromo-N-(2-chloro-5-(dimethylcarbamoyl)phenyl)-4,5-dihydrobenzo[b]thieno[2,3-d]oxepine-2-carboxamide 

Relevant academic research and scientific papers

PYRIDO PYRIMIDINES

Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.

CARBOXYLIC ACID ARYL AMIDES

Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer.

Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform

Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3K has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3K vs PI3K selectivity for two chemical series. In the thienopyrimidine series of inhibitors, we propose that select ligands achieve selectivity derived from a hydrogen bonding interaction with Arg770 of PI3K that is not attained with the corresponding Lys777 of PI3K. In the benzoxepin series of inhibitors, the selectivity observed can be rationalized by the difference in electrostatic potential between the two isoforms in a given region rather than any specific interaction.