107367-81-7

Upstream product

• 107367-72-6 4-hydroxymethyl-2-((E)-2-phenyl-1-ethenyl)-1,3-oxazole 
• 107367-65-7 2-trans-styryl-oxazole-4-carboxylic acid 
• 102-92-1 Cinnamoyl chloride 
• 621-79-4 cinnamamide 
• 534-07-6 1,3-Dichloroacetone 
• 140-10-3 (E)-3-phenylacrylic acid 
• 139684-24-5 N-cinnamoyl-L-serine methyl ester 
• 263404-00-8 methyl 2-styryl-2-oxazoline-4-carboxylate 
• 140381-00-6 methyl 2-[(E)-2-phenylethenyl]-1,3-oxazole-4-carboxylate 

Downstream Products

• 178609-93-3 5-[3-[3-methoxy-4-[2-[(E)-styryl]-4-oxazolylmethoxy]phenyl]propyl]-2,4-oxazolidinedione 
• 107367-72-6 4-hydroxymethyl-2-((E)-2-phenyl-1-ethenyl)-1,3-oxazole 
• 107367-95-3 [2-((E)-Styryl)-oxazol-4-yl]-acetic acid 

Relevant academic research and scientific papers

Identification of a novel toxicophore in anti-cancer chemotherapeutics that targets mitochondrial respiratory complex i

Disruption of mitochondrial function selectively targets tumour cells that are dependent on oxidative phosphorylation. However, due to their high energy demands, cardiac cells are disproportionately targeted by mitochondrial toxins resulting in a loss of cardiac function. An analysis of the effects of mubritinib on cardiac cells showed that this drug did not inhibit HER2 as reported, but directly inhibits mitochondrial respiratory complex I, reducing cardiac-cell beat rate, with prolonged exposure resulting in cell death. We used a library of chemical variants of mubritinib and showed that modifying the 1H-1,2,3-triazole altered complex I inhibition, identifying the heterocyclic 1,3-nitrogen motif as the toxicophore. The same toxicophore is present in a second anti-cancer therapeutic carboxyamidotriazole (CAI) and we demonstrate that CAI also functions through complex I inhibition, mediated by the toxicophore. Complex I inhibition is directly linked to anti-cancer cell activity, with toxicophore modification ablating the desired effects of these compounds on cancer cell proliferation and apoptosis.

Oxazolidinedione derivatives, their production and use

2,4-Oxazolidinedione derivative represented by the formula: STR1 wherein R stands for an optionally substituted hydrocarbon residue or heterocyclic group; Y stands for a group represented by --CO--, --CH(OH)-- or --NR3 -- (wherein R3 stands for an optionally substituted alkyl group); m is 0 or 1; n is 0, 1 or 2; A stands for a C1-7 divalent aliphatic hydrocarbon group; R1 stands for hydrogen or an alkyl group; ring E stands for a benzene ring having 1 or 2 substituents; L and M respectively stand for hydrogen, or L and M may optionally be combined with each other to form a bond; with a proviso that the partial formula: STR2 does not include the formula: STR3 wherein R' stands for an alkyl group; or a salt thereof, which has excellent actions of lowering blood sugar and lipid in blood.