74620-48-7

Upstream product

• 555-16-8 4-nitrobenzaldehdye 
• 54-12-6 Trp 
• 153-94-6 D-tryptophan 

Downstream Products

• 82789-21-7 methyl-1-(4-nitrophenyl)-2,3,4,9-tetrahydro-1H-β-carboline-3-carboxylate 
• 942217-52-9 1-(4-nitrophenyl)-β-carboline-3-carboxylic acid methyl ester 
• 942217-37-0 1-(4-nitrophenyl)-9H-β-carboline-3-carboxylic acid 
• 1381770-99-5 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-4-methoxybenzamide 
• 771533-59-6 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)acetamide 
• 1381771-15-8 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-4-cyanobenzamide 
• 1381771-14-7 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-4-(trifluoromethyl)benzamide 
• 1381771-13-6 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-2,5-dimethylfuran-3-carboxamide 
• 1381771-11-4 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)dodecanamide 
• 1381771-10-3 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)pentanamide 
• 1381771-09-0 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-4-methylbenzamide 
• 1381771-08-9 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-4-tert-butylbenzamide 
• 1381771-07-8 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-3,4-difluorobenzamide 
• 1381771-06-7 N-(4-(9H-pyrido[3,4-b]indol-1-yl)phenyl)-2,4-difluorobenzamide 

Relevant academic research and scientific papers

Discovery of pyridoindole derivatives as potential inhibitors for phosphodiesterase 5A: in silico and in?vivo studies

The aim of this work was to synthesise derivatives from identified plant based pyridoindole lead scaffold, and to assess phosphodiesterase 5A inhibitory potential by in silico and in?vivo. Pyridoindole derivatives were synthesised by using six-stage reactor. In silico screening was carried out by grip-based docking methodology. In step-I, tryptophan as a starting material was reacted with different aldehydes and ketones to obtain 11 molecules. In step-II, obtained molecules were reacted with ethanol and benzyl alcohols to obtain D1 to D22 derivatives. In silico investigation resulted in best three molecules D12, D4 and D8 with promising BE score. Oral acute toxicity study of selected molecules resulted in LD50 value 500 mg/kg in rats. The result of in?vivo antihypertensive study shown that molecule D12 was found to be the best antihypertensive lead molecule. This study could be a best platform to tailor novel biomolecules for inhibiting phosphodiesterase 5A enzyme in hypertension management.

β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma

In an effort to develop anticancer agents that may overcome drug resistance, the number one reason in caner death, we have developed a series of novel hybrids of β-carboline and N-hydroxycinnamamide as histone deacetylase (HDAC) inhibitors. Most of the hybrids 13a-p showed strong antiproliferative effects with low-micromolar IC50 values against four human cancer cells. The most potent compound of series 13p exhibited high HDAC1/6 inhibitory effects, and also increased the acetylation levels of histone H3, H4 and α-tubulin. Importantly, 13p demonstrated high anticancer potency against drug-sensitive HepG2 and Bel7402 cells and drug-resistant Bel7402/5FU cells. Hybrid 13p triggered significant apoptosis by regulating apoptotic relative proteins expression in these Bel7402/5FU cells. Finally, 13p induced a substantial amount of autophagic flux activity by the accretion of the expression of LC3-II and the degeneration of expression of p62 and LC3-I in Bel7402/5FU cells. Overall, 13p is a novel β-carboline/N-hydroxycinnamamide hybrid with significant anticancer potency that warrants further evaluation for the treatment of drug-resistant hepatocellular carcinoma.

Synthesis and anti-leishmanial activity of 1-aryl-β-carboline derivatives against Leishmania donovani

β-carbolines from various natural and synthetic sources have been known to show diverse biological activities. As a part of our current ongoing project to search for potent natural product-derived anti-leishmanial compounds, we have synthesized a series of substituted 1-aryl-β-carboline derivatives. A total of 22 compounds were synthesized and tested in vitro against Leishmania donovani, out of which 6 compounds (4, 5, 10, 11, 19 and 22) showed notably more activity than the standard miltefosine (IC50 12.07 ± 0.82 μM), with compound 4 being the most potent (IC 50 2.16 ± 0.26 μM).

Kinesin inhibitors

The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.

β-Carbolines as specific inhibitors of cyclin-dependent kinases

Harmine (3), 7-fluoro-1-methyl β-carboline (35) and 1-(5-methyl-imidazol-4-yl) β-carboline (41) were potent and specific inhibitors of cyclin-dependent kinases. The degree of aromaticity of the tricyclic ring and the positioning of substituents are important for inhibitory activity. While most β-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) β-carbolines.