A scientific open access journal in the field of synthetic organic chemistry and polymers
Organic CommunicationsA scientific open access journal in the field of synthetic organic chemistry and polymers
Synthesis and biological evaluation of new 4-thiazolidinone derivatives of flurbiprofen
In this study, the synthesis and characterization of 2-(2-fluorobiphenyl-4-yl)-N´-[(substituted methylene]propanehydrazides (3a-s) and 2-(2-fluoro-[1,1'-biphenyl]-4-yl)-N-(5-methyl-2-(substituted aryl)-4-oxothiazolidin-3-yl)propanamides (4a-s) are described and also the antiproliferative effect of the compounds on HT-29, HeLa, A549 and MCF-7 cancer cell lines is investigated. Additionally, mouse embryonic fibroblast cells NIH3T3 were also evaluated to determine the selectivity. The results showed that the identified compounds did not cause any toxicity against NIH3T3 cell line. Moreover, N-(2-(3,5-Bis(trifluoromethyl)phenyl)-5-methyl-4-oxothiazolidin-3-yl)-2-(2-fluoro-[1,1'-biphenyl]-4-yl)propanamide (4h) had the most growth inhibitory effect (55.97% inhibition) on HT-29 colorectal adenocarcinoma cell line. The results obtained from the study show that the compound 4h, which has no cytotoxic effect on normal cells, may be an alternative in the treatment of colon cancer.DOI http://doi.org/10.25135/acg.oc.144.2212.2653 Keywords Hydrazone 4-thiazolidinone MTT antiproliferative activity flurbiprofen Available online: March 13, 2023 DETAILS DOWNLOAD PDF © ACG Publications. All rights reserved.
Synthesis of some piperazine/piperidine amides of chromone-2-carboxylic acid as potential soluble epoxide hydrolase (sEH) inhibitors
Inhibition of soluble epoxide hydrolase (sEH) is implicated as a new therapeutic approach against inflammatory disorders in the context of metabolic and cardiovascular diseases. In the course of our ongoing research on sEH inhibitors, we synthesized novel piperididine/piperazine amide derivatives of the chromone-2-carboxylic acid, and evaluated their inhibitory properties against human sEH. The chemical structures of the target compounds (2-5, 7-9) were elucidated by means of 1H-NMR, 13C-NMR and HRMS spectra. Initial screening of final compounds against sEH at a final concentration of 10 micromolar led to the identification of compound 7, which inhibited sEH activity in a concentration-dependent manner with an IC50 = 1.75 micromolar. Therefore, this chromen-2-amide derivative 7 decorated with benzyl piperidine on the amide side can be regarded as a novel lead structure, which pave the way of developing new analogues with improved inhibitory activities against sEH.DOI http://doi.org/10.25135/acg.oc.145.2302.2705 Keywords fluorometric inhibition piperazine piperidine soluble epoxide hydrolase Available online: March 10, 2023 DETAILS DOWNLOAD PDF © ACG Publications. All rights reserved.
Molecular docking and antioxidant activity studies of imidodithiocarbonate derivatives containing pyrimidine
Imidodithiocarbonate derivatives containing pyrimidine ring, potentially functional molecules were synthesized and characterized. FTIR, 1H NMR and 13C NMR spectroscopy and elemental analysis methods were used for characterization. The obtained compounds were screened for their antioxidant capacity using DPPH (1,1-diphenyl-2-picrylhydraziyl) free radical-scaving and ABTS (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonicacid) assays. The possible interactions between the molecular docking calculations of the synthesized imidodithiocarbonate derivatives and their binding potentials to the active sites of target enzymes.DOI http://doi.org/10.25135/acg.oc.143.2212.2658 Keywords Pyrimidine imidodithiocarbonate molecular docking antioxidant activity Available online: February 28, 2023 DETAILS DOWNLOAD PDF © ACG Publications. All rights reserved.