1684386-71-7

Usage

Uses

1. Used in Pharmaceutical Industry:
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-(4-[(2,2-difluoroacetamido)methyl]phenylmethyl)-2,4-dihydroxybenzamide is used as a potential therapeutic agent for targeting pyruvate dehydrogenase kinase (PDK). As a novel pan-isoform ATP competitive inhibitor, it can modulate the activity of PDK, which plays a crucial role in cellular metabolism and energy production. Inhibition of PDK has been associated with the regulation of various cellular processes, including cell growth, survival, and apoptosis, making it a promising target for the development of anti-cancer and other therapeutic agents.
2. Used in Drug Delivery Systems:
Similar to gallotannin, N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-(4-[(2,2-difluoroacetamido)methyl]phenylmethyl)-2,4-dihydroxybenzamide may also benefit from novel drug delivery systems to enhance its bioavailability, delivery, and therapeutic outcomes. By employing carriers such as organic and metallic nanoparticles, the compound's efficacy against specific biological targets can be improved, potentially leading to more effective treatments for various diseases.

Upstream product

• 1780-31-0 2,6-dichloro-5-methylpyrimidine 
• 330793-01-6 (4-tert-butoxycarbonylaminophenyl)boronic acid pinacol ester 
• 156866-52-3 tert-butyl N-(4-formylbenzyl)carbamate 
• 121903-70-6 benzyl 2,4-bis(benzyloxy)benzoate 
• 121903-71-7 2,4-bis(benzyloxy)benzoyl chloride 
• 89-86-1 4-hydroxysalicylic acid 
• 85593-77-7 2,4-bis(benzyloxy)benzoic acid 

Relevant academic research and scientific papers

Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase

Libraries of nonpurified resorcinol amide derivatives were screened by surface plasmon resonance (SPR) to determine the binding dissociation constant (off-rate, kd) for compounds binding to the pyruvate dehydrogenase kinase (PDHK) enzyme. Parallel off-rate measurements against HSP90 and application of structure-based drug design enabled rapid hit to lead progression in a program to identify pan-isoform ATP-competitive inhibitors of PDHK. Lead optimization identified selective sub-100-nM inhibitors of the enzyme which significantly reduced phosphorylation of the E1α subunit in the PC3 cancer cell line in vitro.

RESORCINOL N-ARYL AMIDE COMPOUNDS, FOR USE AS PYRUVATE DEHYDROGENASE KINASE INHIBITORS

A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: Y is –CONR1- or optionally substituted arylene or optionally substituted heteroarylene; R1 is H, Cl, F, CH3 or CF3; 10 each R4 is independently H, CH3 or F; R5 is H or CH3; and each R2 and R6 is independently (Alk)n-Rn-(Alk)n-Rn-(Alk)n-X; The compounds of the invention are useful as resorcinol N-aryl amide (NAA) compounds, which are suitable for use as PDK inhibitors, for example for 15 inhibition of cancer cell proliferation.