1638845-60-9

Upstream product

• 100-63-0 phenylhydrazine 
• 308103-40-4 (2-acetylphenyl)boronic acid 
• 118-93-4 o-hydroxyacetophenone 

Downstream Products

• 19726-10-4 2-(1-phenyl-5-phenyl-1H-pyrazol-3-yl)phenol 
• 142029-25-2 (2-O-C₆H₄C(CH₃)NNHC₆H₅)2copper 
• 1423043-90-6 2-[1-phenyl-4-(2H-tetrazol-5-yl)-1H-pyrazol-3-yl]phenol 
• 1421356-02-6 2-(3-(methylsulfonyl)-1H-indol-2-yl)phenol 
• 1421356-00-4 2-(1H-indol-2-yl)phenyl methanesulfonate 
• 1421355-98-7 2-(1-methyl-1H-indol-2-yl)phenyl trifluoromethanesulfonate 
• 1421355-85-2 2-(3-(trifluoromethylsulfonyl)-1H-indol-2-yl)phenol 
• 1421355-72-7 2-(1H-indol-2-yl)phenyl trifluoromethanesulfonate 
• 1393711-68-6 4-(3-(2-hydroxyphenyl)-1-phenyl-1H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarbonitrile 
• 833-31-8 4-methyl-2-oxo-2H-chromene-3-carboxylic acid 

Relevant academic research and scientific papers

Curcumin-I Knoevenagel's condensates and their Schiff's bases as anticancer agents: Synthesis, pharmacological and simulation studies

Pyrazolealdehydes (4a-d), Knoevenagel's condensates (5a-d) and Schiff's bases (6a-d) of curcumin-I were synthesized, purified and characterized. Hemolysis assays, cell line activities, DNA bindings and docking studies were carried out. These compounds were lesser hemolytic than standard drug doxorubicin. Minimum cell viability (MCF-7; wild) observed was 59% (1.0 μg/mL) whereas the DNA binding constants ranged from 1.4 × 10 3 to 8.1 × 105 M-1. The docking energies varied from -7.30 to -13.4 kcal/mol. It has been observed that DNA-compound adducts were stabilized by three governing forces (Van der Wall's, H-bonding and electrostatic attractions). It has also been observed that compounds 4a-d preferred to enter minor groove while 5a-d and 6a-d interacted with major grooves of DNA. The anticancer activities of the reported compounds might be due to their interactions with DNA. These results indicated the bright future of the reported compounds as anticancer agents.

The preparation of 2-(1-phenyl-5-phenyl or 5-substituted phenyl-1H- pyrazol-3-yl)phenols from trilithiated 2'-hydroxyacetophenone phenylhydrazone and aromatic esters

2'-Hydroxyacetophenone phenylhydrazone was trilithiated with excess lithium diisopropylamide, and the resulting trianion-type intermediate was condensed with a variety of aromatic esters followed by acid cyclization to 2-(1-phenyl-5-phenyl or 5-substitute

Synthesis and Antimicrobial Evaluation of Novel Pyrazole-Annulated Oxygen-Containing Macrocycles

[Figure not available: see fulltext.] An efficient approach to the synthesis of fused pyrazole-annulated macrocycles has been demonstrated. Vilsmeier–Haack reaction of substituted o-hydroxyacetophenones with phenyl hydrazine followed by reduction of the r

Synthesis and characterization of hydrazone and azine derivatives of bis(cyclopentadienyI) titanium(IV)

Pentacoordinated hydrazone and azine derivatives of bis(cyclopentadienyl)titanium(IV) of the type {equation presented}, have been prepared. The products were characterized by chemical analyses, elec- trical conductance, IR, 1H NMR, and electronic spectral studies. Some hydrazone complexes and a few azine com- plexes of titanium have been studied.' ' However, no systematic study on their organometallic derivatives is available. In view of the versatile chelating ability, widespread applications and lack of data involving organometallic derivatives of titanium, it has been considered of interest to study the reactions of Cp2TiCl2 with the title ligands.

Diazaborines Are a Versatile Platform to Develop ROS-Responsive Antibody Drug Conjugates**

Antibody–drug conjugates (ADCs) are a new class of therapeutics that combine the lethality of potent cytotoxic drugs with the targeting ability of antibodies to selectively deliver drugs to cancer cells. In this study we show for the first time the synthesis of a reactive-oxygen-species (ROS)-responsive ADC (VL-DAB31-SN-38) that is highly selective and cytotoxic to B-cell lymphoma (CLBL-1 cell line, IC50 value of 54.1 nM). The synthesis of this ADC was possible due to the discovery that diazaborines (DABs) are a very effective ROS-responsive unit that are also very stable in buffer and in plasma. DFT calculations performed on this system revealed a favorable energetic profile (ΔGR=?74.3 kcal mol?1) similar to the oxidation mechanism of aromatic boronic acids. DABs’ very fast formation rate and modularity enabled the construction of different ROS-responsive linkers featuring self-immolative modules, bioorthogonal functions, and bioconjugation handles. These structures were used in the site-selective functionalization of a VL antibody domain and in the construction of the homogeneous ADC.

New library of pyrazole–imidazo[1,2-α]pyridine molecular conjugates: Synthesis, antibacterial activity and molecular docking studies

A library of novel pyrazole–imidazo[1,2-α]pyridine scaffolds was designed and synthesized through a one-pot three-component tandem reaction. The structures of synthesized conjugates were confirmed by spectroscopic techniques (NMR, IR and HRMS). In vitro antibacterial evaluation of the twelve synthesized molecules (7a, 8a–k) against methicillin-resistant Staphylococcus aureus and normal strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumonia and Pseudomonas aeruginosa established 8b, 8d, 8e, 8h and 8i as potent antibacterial agents with superior minimum bactericidal concentration, compared with standard drug ciprofloxacin. Molecular docking studies of all active compounds into the binding site of glucosamine-6-phosphate synthase were further performed in order to have a comprehensive understanding of putative binding modes within the active sites of the receptor.

Ultrasonic assisted synthesis of 2, 3-dihydroquinazolin-4(1H)-ones involving three-component reaction of isatoic anhydride, amines and pyrazole carbaldehydes catalyzed by [?-fe2o3?hap-So3H]

The combination of [?-Fe2O3?HAp-SO3H] as a catalyst and ultrasonic effect catalyzed the synthesis of diverse derivatives of 2, 3-dihydroquinazolin-4(1H)-ones which is reported in this study. The products were synthesized via the one-pot three-component reaction of isatoic anhydride, amines and pyrazole carbaldehydes in water: EtOH catalyzed by recoverable [?-Fe2O3?HAp-SO3H]. This paper conducted an investigation of the effect of various solvents, temperatures and catalysts on the reactions. Short reaction times, mild reaction conditions, simple work-up, the desired yields and the use of an appropriate catalyst are the advantages of this novel method. The new derivatives were validated by using FT-IR,1HNMR, and13CNMR. Moreover, the synthesized compounds were screened for their an-timicrobial activity against bacterial strains.

AlCl3·6H2O-catalyzed Schiff-base reaction between aryl ketones and aromatic acylhydrazines/hydrazines in water

Abstract: Schiff-bases have important applications in the field of analysis, biomedicine, as well as material sciences. Hydrazones and acylhydrazones are two representative types of Schiff-bases. In this study, a green synthesis of aromatic hydrazones and

Synthesis and Antimicrobial Activities of Novel 2-[substituted-1H-pyrazol-4-yl] Benzothiazoles, Benzoxazoles, and Benzimidazoles

In an endeavor to find a new class of antimicrobial agents, a series of novel substituted benzimidazole, benzoxazole, and benzothiazole derivatives 6 containing pyrazole moiety have been synthesized by reaction of 3-aryl-4-formyl pyrazole 4 with substitut

Identification of novel pyrazole-rhodanine hybrid scaffolds as potent inhibitors of aldose reductase: Design, synthesis, biological evaluation and molecular docking analysis

In an effort to develop a new class of potent aldose reductase inhibitors, a series of 1,3-diarylpyrazole assimilated 3-substituted 4-oxo-2-thioxo-1,3-thiazolidines (9a-n) was designed, and synthesized in good to excellent yields by a pharmacophore integr