72470-43-0

Upstream product

• 181135-43-3 methyl 2-amino-3-N-benzoylaminobenzoate 
• 5337-09-7 2-bromo-3-nitro-benzoic acid methyl ester 
• 107582-20-7 2,3-diaminobenzoic acid methyl ester 
• 100-52-7 benzaldehyde 
• 65-85-0 benzoic acid 
• 95067-27-9 2-acetylamino-3-nitro-benzoic acid methyl ester 
• 57113-91-4 methyl 3-nitroanthranilate 
• 98-88-4 benzoyl chloride 
• 100-46-9 benzylamine 

Downstream Products

• 72470-44-1 NU₁₀₇₀ 
• 579525-37-4 1-[2-(trimethylsilyl)ethoxymethyl]-2-phenylbenzimidazole-4-carboxylic acid methyl ester 
• 579525-38-5 1-[2-(trimethylsilyl)ethoxymethyl]-2-phenylbenzimidazole-7-carboxylic acid methyl ester 
• 66630-72-6 2-Phenyl-4-benzimidazolylcarboxylic acid 
• 1446250-90-3 C₂₈H₃₈N₆O₄S 
• 579525-39-6 1-[2-(trimethylsilyl)ethoxymethyl]-2-phenylbenzimidazole-4-methanol 

Relevant academic research and scientific papers

An efficient synthesis, characterization and biological activity of novel Schiff bases of 2-aryl-1H-benzo[d]imidazole-4-carbohydrazide derivatives

A series of N′-aryllidene-2-aryl-1H-benzo[d]imidazole-4-carbohydrazide (Schiff bases) 3a1-3d4 were synthesized by condensation reaction of 2-aryl-1H-benzo[d]imidazole-4-carbohydrazide (2a-2d) with substituted aromatic aldehyde. The c

ANTI-MALIGNANT TUMOR AGENT COMPOSITION

To provide a satisfactory anticancer agent composition suppressing the growth of cancer (malignant tumor) reliably and hardly causing side effects, the present invention is directed to an anticancer agent composition including the following agents as active ingredient; a LAT1 inhibitor, and one or more agents selected from the group consisting of an alkylating agent, a platinum-based antineoplastic agent, an anti-metabolite, a topoisomerase inhibitor, an anti-microtubule polymerizing agent, a hormonal agent, an anti-microtubule depolymerizing agent, an anticancer antibiotic, and a molecular targeted agent.

Discovery of TD-8954, a clinical stage 5-HT4 receptor agonist with gastrointestinal prokinetic properties

The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and moderate-to-high intrinsic activity relative to that of 5-HT. Consistent with our previously described multivalent design approach to this target, subsequent optimization of the linker and secondary binding group regions of the series afforded compound 18 (TD-8954), a potent and selective 5-HT4 receptor agonist in vitro with demonstrated prokinetic activity in multiple species.

Palladium-catalyzed N-heteroannulation of N-allyl- or N-benzyl-2-nitrobenzenamines: synthesis of 2-substituted benzimidazoles

A palladium-catalyzed reductive N-heteroannulation of N-allyl- or N-benzyl-2-nitrobenzenamines, using carbon monoxide as the ultimate reducing agent, affording 2-substituted benzimidazoles has been developed.

AROMATIC AMINO ACID DERIVATIVES AND MEDICINAL COMPOSITIONS

An aromatic amino acid derivative represented by the formula ( I ) or its pharmacologically acceptable salt: wherein,R1 is a hydrogen atom or an amino-protecting group,R2 is a halogen atom or an alkyl, aralkyl or aryl group,R3 is 1○ a hydrogen atom, 2○ an aroylamino group, 3○ a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. 4○ a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, 5○ an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, 6○ an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; 1 is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5. This compound can inhibit a transporter (LAT1) of essential amino acid which is one of main nutrition for cancer cells and accordingly cause drain of the essential amino acid on the cancer cells and finally can prohibit the multiplication of cancer cells.

Benzimidazole compounds

Benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

Novel benzimidazole and quinazolinone inhibitors of the DNA repair enzyme Poly(ADP-ribose)polymerase

Two novel series of inhibitors of the DNA repair enzyme poly(ADP-ribose)polymerase (PARP) were synthesized and evaluated for biological activity. In the benzimidazole-4-carboxamide series, the carbamoyl function was restricted into the putative biologically active conformation via an intramolecular hydrogen bond, while for quinazolin-4-[3H]-ones this was achieved by incorporation of the group into a heterocyclic ring. For both series of compounds, syntheses involved acylation of substituted anthranilic acid derivatives, followed by acid- or base-catalysed cyclization. 8-Hydroxyquinazolin-4-[3H]-ones were prepared from the corresponding 8-methoxy compounds by dealkylation with boron tribromide. PARP inhibitory activity was determined in permeabilized L1210 murine leukaemia cells, in comparison with the established inhibitor 3-hydroxybenzamide (IC50 = 8.3 μM). For both series, inhibitory activity varied with the nature of the 2-substituent, with benzimidazole-4-carboxamides proving approximately tenfold more potent than the previously prepared benzoxazole-4-carboxamides. 2-Arylbenzimidazoles were especially active, and 2-(4-methoxyphenyl)benzimidazole-4-carboxamide (IC50 = 60 nM) is the most potent PARP inhibitor reported to date. In the quinazolinone series, a 2-(4-nitrophenyl) substituent, and either an 8-methyl or 8-hydroxy group conferred potent inhibitory activity, with IC50 values of 0.13 and 0.23 μM, respectively, being observed.