855839-06-4

Upstream product

• 72221-04-6 2,4-Diacetyl-3,5-dimethoxy-phenol 
• 500-99-2 3,5-dimethoxyphenol 
• 108-24-7 acetic anhydride 
• 90-24-4 2-hydroxy-4,6-dimethoxyacetophenone 
• 7647-01-0 hydrogenchloride 
• 7446-70-0 aluminium trichloride 
• 60-29-7 diethyl ether 
• 75-05-8 acetonitrile 
• 621-23-8 1,2,3-trimethoxybenzene 
• 75-36-5 acetyl chloride 
• 860688-04-6 2,4-diacetyl-1-benzyloxy-3,5-dimethoxy-benzene 
• 2161-86-6 2,4-diacetylphloroglucinol 
• 74-88-4 methyl iodide 

Relevant academic research and scientific papers

Synthesis, biological evaluation and molecular docking studies of bis-chalcone derivatives as xanthine oxidase inhibitors and anticancer agents

In this study, a series of B-ring fluoro substituted bis-chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and evaluated for their ability to inhibit xanthine oxidase (XO) and growth inhibitory activity against MCF-7 and Caco

Design, synthesis and biological evaluation of novel bischalcone derivatives as potential anticancer agents

Building on our previous work that discovered chalcone as a promising pharmacophore for anticancer activity, we have various other chalcone derivatives and have synthesized a series of novel bischalcone to explore their anticancer activity. Among all tested compounds, compounds 6a, 6b, and 6c showed the highest antiproliferative activity against A-549 cancer cell lines with the average IC50 values of 4.18, 4.52, and 5.05 μM, respectively. Moreover, compound 6c showed high antiproliferative activity against the Caco-2 cell line; thus, it was 2- and 4-fold more active than the reference compounds, i.e., methotrexate and capecitabine. Compound 6a also induced cell-cycle arrest in the S phase, whereas compounds 6b and 6c were observed to stop at the G0/G1 phase. Thereafter, we evaluated that compound 6c also had the highest apoptosis/necrosis ratio than other compounds and the standard compound. The anticancer property of the 6c was also supported by molecular docking studies carried out on the EGFR and HER2 receptors. Overall, we expect that these compounds can be further developed for the potential treatment of lung cancer.

Multi-substituted aromatic diketone compound and its preparation method and application (by machine translation)

The invention of the formula (I) of the said multi-substituted aromatic diketone compound and its preparation and application. Formula (I) in R 1 formula (I-1), type (I-2) or a formula (I-3) substituent, R 2 to-H, -F, -Cl, -Br, -CH 3 or-OCH 3. When the R 1 formula (I-1) time, the method of the invention is to 2,4-di-hydroxy acetophenone as raw materials, and the bromine acetaldehyde compressed ethylene glycol reaction to obtain 1 - (4 - (2,2-methoxyethoxy) - 2-hydroxy-phenyl) ethanone, then the ring, and aryl acyl chloride reaction, the rearranged under alkaline conditions to obtain multi-substituted aromatic diketone compound. When the R 1 (I-2) for the time, the method of this invention and R 1 (I-1) is basically the same as the. When the R 1 formula (I-3) time, the method of the invention is to to phloroglucinol as raw materials, by methylation of 1, 3, 5-trimethoxy, by reaction with acetyl chloride 1,1 ˊ - (2-hydroxy -4,6-dimethoxy -1,3-phenylene) b ethanone, then the aryl acyl chloride reaction, the rearranged under alkaline conditions to obtain multi-substituted aromatic diketone compound. Compound of the present invention, to HIV-1 integrase inhibiting effect. (by machine translation)

Design, synthesis and biological activity of aromatic diketone derivatives as HIV-1 integrase inhibitors

A series of aromatic diketone derivatives were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated to determine their ability to inhibit the strand transfer process of HIV-1 integrase. The results indicate that (Z)-1-(3-acetyl-2-hydroxy-4,6-dimethoxyphenyl)-3-hydroxy-3-(substituted)phenylprop-2-en-1-one (5a-5d) can moderately inhibit HIV-1 integrase. The cyclization and condensation products (6a-6c and 7e-7f) of compounds 5a-5d show poor inhibitory activity against HIV-1 integrase. The molecular docking results indicate that the different types of compounds act on HIV-1 integrase in different ways, and these results can explain the differences in the inhibitory activities.