29838-16-2

Upstream product

• 123-08-0 4-hydroxy-benzaldehyde 
• 122-00-9 para-methylacetophenone 
• 52820-26-5 4-hydroxyphenylacryloyl chloride 
• 108-88-3 toluene 

Downstream Products

• 1462341-36-1 C₂₂H₁₈N₂O 
• 1246618-04-1 4-(1-acetyl-3-4'-methylphenyl-2-pyrazolin-5-yl)phenol 

Relevant academic research and scientific papers

Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia

Based on hit-likeness and chemical diversity, a number of chalcones and chalcone-mimetic compounds were selected as putative Notch inhibitors. The evaluation of the antiproliferative effect combined with the inhibition of Notch1 expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.

Antibacterial and anti-inflammatory activity of valproic acid-pyrazole conjugates as a potential agent against periodontitis

Periodontitis is a serious global concern. Therefore, in the present study, we intend to synthesize novel valproic-acid pyrazole conjugates as a novel agent against periodontitis. The molecules were developed in a facile synthetic route and obtained in ex

Lewis acid catalyst system for Claisen-Schmidt reaction under solvent free condition

Ca(OTf)2 in combination with NBu4.BF4 was established to function as an efficient catalyst system for one-pot Claisen-Schmidt condensation under neat conditions. Substituted acetophenones and benzaldehydes were coupled in situ to afford their corresponding chalcones in excellent yields. The method, with a broad range of substrate tolerance and mild operational conditions can produce assorted chalcone derivatives in moderate to high yields from easily accessible starting materials.

Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation

Four new series of aromatic sulfamates were synthesized and investigated for the inhibition of four human (h) isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), hCA I, II, IX, and XII. The reported derivatives, obtained by a sulfamoylation reaction of the corresponding phenolic precursors, bear 3,5-diarylpyrazoline moieties as spacers between the benzenesulfamate fragment which binds the zinc ion from the active site, and the tail of the inhibitor. Pyrazolines are biologically privileged scaffolds, endowed with versatile biological activity, such as an anti-proliferative action. The derivatives were tested for the inhibition of the cytosolic, hCA I and II (off target isoforms) and the trans-membrane, tumor-associated hCA IX and XII enzymes (anticancer drug targets). Generally, hCA I was not effectively inhibited, whereas many low nanomolar inhibitors were evidenced against hCA II (KIs in the range of 0.42–90.1 nM), IX (KIs in the range of 0.72–63.6 nM), and XII (KIs in the range of 0.88–85.2 nM). The best substitution fragments at the pyrazoline ring included for CA II a 4-sulfamic group on the 3-aryl and halogens on the 5-aryl or a methoxy group on the 3-aryl and a 4-sulfamate group on the 5-aryl; for CA IX and CA XII they included the sulfamic group on the 3- or 4-position of the 5-aryl and an electronwithdrawing group on the 4-postion of the 3-aryl ring.

Monofunctionalized 1,3,5,7-tetraarylazaBODIPYs and their application in the synthesis of AzaBODIPY based conjugates

A series of monofunctionalized 1,3,5,7-tetraarylazaBODIPYs containing functional groups such as p-hydroxymethyl phenyl, p-hydroxyphenyl, p-cyanophenyl, p-nitrophenyl, and p-formylphenyl groups at the 1-position of the azaBODIPY core were synthesized by mi

Microwave-assisted synthesis and bioevaluation of new sulfonamides

In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13C N

Monoamine Oxidase Inhibitory Activity: Methyl- versus Chlorochalcone Derivatives

Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series

Niacin esters of chalcones with tumor-selective properties

Novel series of niacin esters of chalcones 2, 4 and 6 were designed as antineoplastic agents that have the potential to release the chemoprotectant niacin. These enones are cytotoxic to human CD4 +T-lymphocyte Molt 4/C8 and CEM and murine leukemia L1210 cells. Quantitative structure–activity relationship (QSAR) studies of the biodata in series 4 revealed that cytotoxic potency was enhanced by placing electron-repelling groups in one of the aryl rings. The compounds are lethal to HL-60, HSC-2, HSC-3 and HSC-4 neoplasms but less toxic to nonmalignant hepatocyte growth factor, hematopoietic progenitor cell and human periodontal ligament fibroblast cells. Hence, the compounds display tumor-selective toxicity. These chalcones are well tolerated in mice and no overt toxicity was noted. The results establish that in general the compounds in series 2, 4 and 6 have positive characteristics which warrant further studies.

Synthesis and study of antibacterial activity of some 1-phenyl-3-aryl-5-(4- (2-ethanoloxy) phenyl)-1H-pyrazoles

A series of 1-phenyl-3-aryl-5-(4-(2-ethanoloxy) phenyl)-1H-pyrazoles were synthesized from chalcones and studied for their in vitro antibacterial activity. Chalcones i.e., 1-aryl-3-(4-hydroxyphenyl) prop-2-en-1-ones, 1 on reaction with phenyl hydrazine yi

Zinc oxide as a regioselective and heterogeneous catalyst for the synthesis of chalcones at room temperature

Zinc oxide catalyzed synthesis of chalcones has been carried out under solvent-free conditions at room temperature. Activated as well as unactivated aromatics smoothly underwent Friedel-Crafts acylation with α, β-unsaturated acid chlorides furnishing excellent yields of the corresponding chalcones. The zinc oxide can be recovered and reused at least three times without any appreciable loss in activity.