200411-98-9

Upstream product

• 4397-53-9 p-benzyloxybenzaldehyde 
• 118-93-4 o-hydroxyacetophenone 

Downstream Products

• 24271-94-1 1-(2-hydroxyphenyl)-3-(4-hydroxyphenyl)-propan-1-one 
• 102468-65-5 2-(4-(benzyloxy)phenyl)-3-hydroxy-4H-chromen-4-one 
• 1209469-98-6 3-benzyl-2',4-dihydroxychalcone 
• 1209469-97-5 3'-benzyl-4'-hydroxyflavanone 
• 6515-37-3 2-(4-hydroxyphenyl)chroman-4-one 
• 1258439-86-9 C₂₈H₂₄N₂O₂ 
• 95161-87-8 2-[4-(benzyloxy)phenyl]-4H-chromen-4-one 
• 111391-62-9 2-(4-benzyloxy-phenyl)-3-methoxy-chromen-4-one 
• 14919-49-4 3-hydroxy-2-(4-hydroxy-phenyl)-chromen-4-one 
• 111391-31-2 2-(4-hydroxyphenyl)-3-methoxy-4H-chromen-4-one 

Relevant academic research and scientific papers

Novel chalcones and 1,3,5-triphenyl-2-pyrazoline derivatives as antibacterial agents

Novel sixteen chalcones and thirteen 1,3,5-triphenyl-2-pyrazolines were synthesized and characterized using FT-IR, HR-Mass, NMR (1H-NMR, 13C-NMR, 135 DEPT, 1H-1H CoSY and 1H and 13C CoSY) a

Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors against melanoma and non-melanoma skin cancers

Due to hurdles, including resistance, adverse effects, and poor bioavailability, among others linked with existing therapies, there is an urgent unmet need to devise new, safe, and more effective treatment modalities for skin cancers. Herein, a series of flavonol-based derivatives of fisetin, a plant-based flavonoid identified as an anti-tumorigenic agent targeting the mammalian targets of rapamycin (mTOR)-regulated pathways, were synthesized and fully characterized. New potential inhibitors of receptor tyrosine kinases (c-KITs), cyclin-dependent kinase-2 (CDK2), and mTOR, representing attractive therapeutic targets for melanoma and non-melanoma skin cancers (NMSCs) treatment, were identified using inverse-docking, in vitro kinase activity and various cell-based anticancer screening assays. Eleven compounds exhibited significant inhibitory activities greater than the parent molecule against four human skin cancer cell lines, including melanoma (A375 and SK-Mel-28) and NMSCs (A431 and UWBCC1), with IC50 values ranging from 0.12 to 15 μM. Seven compounds were identified as potentially potent single, dual or multi-kinase c-KITs, CDK2, and mTOR kinase inhibitors after inverse-docking and screening against twelve known cancer targets, followed by kinase activity profiling. Moreover, the potent compound F20, and the multi-kinase F9 and F17 targeted compounds, markedly decreased scratch wound closure, colony formation, and heightened expression levels of key cancer-promoting pathway molecular targets c-Kit, CDK2, and mTOR. In addition, these compounds downregulated Bcl-2 levels and upregulated Bax and cleaved caspase-3/7/8 and PARP levels, thus inducing apoptosis of A375 and A431 cells in a dose-dependent manner. Overall, compounds F20, F9 and F17, were identified as promising c-Kit, CDK2 and mTOR inhibitors, worthy of further investigation as therapeutics, or as adjuvants to standard therapies for the control of melanoma and NMSCs.

Design, synthesis, molecular modelling, and in vitro evaluation of tricyclic coumarins against Trypanosoma cruzi

Chagas disease is caused by infection with the parasite protozoan Trypanosoma cruzi and affects about 8 million people in 21 countries in Latin America. The main form of treatment of this disease is still based on the use of two drugs, benznidazole and nifurtimox, which both present low cure rates in the chronic phase and often have serious side-effects. Herein, we describe the synthesis of tricyclic coumarins that were obtained via NHC organocatalysis and evaluation of their trypanocidal activity. Molecular docking studies against trypanosomal enzyme triosephosphate isomerase (TIM) were carried out, as well as a theoretical study of the physicochemical parameters. The tricyclic coumarins were tested in vitro against the intracellular forms of Trypanosoma cruzi. Among the 18 compounds tested, 10 were more active than the reference drug benznidazole. The trypanocidal activity of the lead compound was rationalized by molecular docking study which suggested the strong interaction with the enzyme TIM by T.?cruzi and therefore indicating a possible mode of action. Furthermore, the selectivity index of eight tricyclic coumarins with high anti-T.?cruzi activity was above 50 and thus showing that these lead compounds are viable candidates for further in vivo assays.

2-pyrazoline derivatives in neuropharmacology: Synthesis, adme prediction, molecular docking and in vivo biological evaluation

A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives (PFC-1 to PFC-16) were synthesized in a three step reaction using conventional and microwave assisted green chemistry approach. The synthesized derivatives were characterized and their chemic

3′-Hydroxy-3,4′-dimethoxyflavone blocks tubulin polymerization and is a potent apoptotic inducer in human SK-MEL-1 melanoma cells

Flavonoids are naturally occurring polyphenolic compounds and are among the most promising anticancer agents. A series of flavonols and their 3-methyl ether derivatives were synthesized and assessed for cytotoxicity. It was found that 3′-hydroxy-3,4′-dime

Quantum-chemical analysis of the Algar-Flynn-Oyamada reaction mechanism

This work is devoted to improving the understanding of Algar-Flynn-Oyamada reaction mechanism and the analysis of factors that affect the formation of flavonols. The calculation of thermodynamic parameters for the key reaction steps pointed to a mechanism involving chalcone epoxides as intermediates. A correlation was identified between the nucleophilicity of oxygen atom at position 2' of epoxide anions and the yields of flavonols. An increased charge at the nucleophilic center was shown to reduce the effectiveness of β-cyclization of epoxide anions.

Total synthesis of 3′,3?-binaringenin and related biflavonoids

The synthesis of natural 3++,3?-binaringenin and four related biflavonoids was performed in good overall yield (15-35%) starting from readily available phloroglucinol and 4-hydroxy- or 4-methoxybenzaldehyde. Preliminary results indicate that some of these compounds have an interesting activity against S. aureus. Georg Thieme Verlag Stuttgart.

Structural characterization and cytotoxicity studies of ruthenium(II)-dmso-chloro complexes of chalcone and flavone derivatives

A synthetic precursor cis-[RuIICl2(dmso)4] is complexed separately with 3-(4-benzyloxyphenyl)-1-(2-hydroxylphenyl)-prop-2-en-1-one (L1H) and 2-(4-benzyloxyphenyl)-3hydroxy-chromen-4-one (L2H). The resulting complexes are assigned the composition fac-[RuCl(S-dmso)3(L1)] 1 and fac-[RuCl(S-dmso)3(L2)] 2 using elemental analyses, FAB mass data and spectroscopic (IR, 1H NMR, UV-Vis, emission) spectral properties. The X-ray diffraction analysis shows that complexes self-associate through non-covalent interactions and provide 1D and 2D supramolecular structures. These complexes are assayed for their cytotoxicity studies on Dalton Lymphoma cell lines.