18064-89-6

Upstream product

• 90-24-4 2-hydroxy-4,6-dimethoxyacetophenone 
• 621-23-8 1,2,3-trimethoxybenzene 
• 108-73-6 3,5-dihydroxyphenol 

Downstream Products

• 1159-57-5 3'-bromo-2'-hydroxy-4',6'-dimethoxy-trans-chalcone 
• 3410-83-1 2-hydroxy-3,5-dibromo-4,6-dimethoxyacetophenone 
• 18064-90-9 2-acetoxy-3-bromo-4,6-dimethoxyacetophenone 
• 1159-57-5 1-(3-bromo-4,6-dimethoxy-2-hydroxyphenyl)-3-phenyl-2-propen-1-one 
• 29784-38-1 3-bromo-2,4,6-trimethoxyacetophenone 
• 1149368-10-4 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-nitrophenyl)-2-propen-1-one 
• 1607-73-4 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-methoxyphenyl)-2-propen-1-one 
• 1149368-11-5 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(2-carboxyphenyl)-2-propen-1-one 
• 1149368-09-1 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-butoxyphenyl)-2-propen-1-one 
• 1149368-08-0 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one 
• 1265608-53-4 (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one 
• 1374842-01-9 (2E,4Z)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-5-chloro-5-(3,4-dimethoxyphenyl)penta-2,4-dien-1-one 
• 1374843-02-3 (2E,4Z)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-5-chloro-5-(3-chloro phenyl)penta-2,4-dien-1-one 
• 1374842-15-5 (2E,4Z)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-5-chloro-5-(4-chloro phenyl)penta-2,4-dien-1-one 

Relevant academic research and scientific papers

The first synthesis of podocarflavone A and its analogs and evaluation of their antimycobacterial potential against Mycobacterium tuberculosis with the support of virtual screening

The first synthetic route developed for Podocarflavone A reported from Podocarpus macrophyllus and its analogs in 7 steps. Computational analysis for binding with the pantothenate kinase (3AVO) of Mycobacterium tuberculosis showed their docking score (ds) in the range of ?8.9 to ?9.3 Kcal/mol. MD simulations delineated the stability of the protein-ligand complexes in the TIP3P model. MMGBSA and MMPBSA values of 8d were ?42.46 Kcal/mol and ?14.58 Kcal/mol, respectively. Further in-vitro antitubercular screening of compounds 8a, 8d, and 8e against M. tuberculosis H37Ra using XRMA protocol exhibited promising antimycobacterial activity with IC50 values 21.82μg/mL, 15.55 μg/mL, and 16.56 μg/mL, respectively. Compounds 8a, 8d, and 8e showed antibacterial activity with IC50 values 41.56 μg/mL, 24.72 μg/mL, and 72.45 μg/mL respectively against the Staphylococcus aureus. 8a and 8d showed inhibition with IC50 values 39.6 μg/mL and 27.64 μg/mL, respectively, against Bacillus subtilis. The present study could help in the further development of lead molecules against tuberculosis.

Synthesis and biological evaluation of novel series of chalcone derivatives as inhibitors of cyclooxygenase and LPS-induced TNF-α with potent antioxidant properties

Novel series of chalcones were synthesized and were evaluated as possible anti-inflammatory agents targeting the cyclooxygenase-1 and 2 (COX-1 and 2), β-glucuronidase, trypsin, and TNF-α. Amongst the tested chalcones the compound 4k was found to be most effective inhibitor of TNF-α exhibiting 85% inhibition activity (IC50 = 0.1 μM). The compounds 4a, 4f, 4l, and 4m were found to inhibit the COX-1 activity in as a range of 79.95-68.47% and COX-2 inhibition ranging 84.45-74.77%. The compounds 4l (81.71%) and 4f (72.10%) were found to be excellent inhibitors of trypsin and β-glucuronidase, respectively. Springer Science+Business Media, LLC 2011.

Synthesis, biological evaluation and in silico study of β-chloro vinyl chalcones as inhibitors of the TNF-α, IL-6 with anticancer and antioxidant activity

A series of novel β-chloro vinyl chalcones have been synthesized from substituted (Z)-3-chloro-3-phenylacraldehydes with 1-(3-bromo-2-hydroxyl-4,6- dimethoxyphenyl)ethanone by Claisen-Schmidt condensation reaction. Compounds were screened for anti-inflammatory, anticancer and antioxidant activity. Compounds 6a, 6d and 6f revealed promising anti-inflammatory activity (87-99 %) with less cytotoxicity (4-9 %) at 10 μM. Compounds 6a, 6d, 6e and 6f having significant anticancer activity (71-83 %). Bioavailability of compounds were checked by in vitro cytotoxicity and confirmed to be nontoxic. Structure activity relationship and in silico drug relevant properties of compounds revealed as potential candidates for future drug discovery study.

Synthesis of 5/-bromo-2/-hydroxy-4,4/,6/-trimethoxychalcone from Garcinia nervosa and of its isomer 3/-bromo-2/-hydroxy-4,4/,6-/trimethoxychalcone

The unambiguous syntheses of the naturally occurring 5'-bromo-2'-hydroxy-4, 4',6'-trimethoxychalcone 1, a constituent of Garcinia nervosa, and its positional isomer 3'-bromo-2'-hydroxy-4,4',6'-trimethoxychalcone 6 are described.