On April 3, 2018, Lamie, Phoebe F.; Philoppes, John N.; Rarova, Lucie published an article.Application In Synthesis of 2-(4-Methylbenzamido)acetic acid The title of the article was Design, synthesis, and biological evaluation of novel 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives as cytotoxic agents and COX-2/LOX inhibitors. And the article contained the following:
A new series of 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives I (R = H, Me; R1 = H, OMe, Cl; X = O, S) was synthesized. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also against normal human skin fibroblasts. Cyclooxygenase (COX)-1, COX-2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX-2 rather than COX-1, and the IC50 values (0.25-1.7 μM) were lower than that of indomethacin (IC50 = 9.47 μM) and somewhat higher than that of celecoxib (IC50 = 0.071 μM). The selectivity index for COX-2 of the oxazole derivative I (R = Me; R1 = OMe; X = O) (SI = 3.67) was nearly equal to that of celecoxib (SI = 3.66). For the LOX inhibitory activity, the new compounds showed IC50 values of 0.02-74.03 μM, while the IC50 of the reference zileuton was 0.83 μM. The most active compound I (R = H; R1 = Cl; X = O) was found to have dual COX-2/LOX activity. All the synthesized compounds were docked inside the active site of the COX-2 and LOX enzymes. They linked to COX-2 through the N atom of the azole scaffold, while C=O of the oxazolone moiety was responsible for the binding to amino acids inside the LOX active site. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Application In Synthesis of 2-(4-Methylbenzamido)acetic acid
The Article related to benzylidene imidazolone preparation antiinflammatory antitumor mol docking human, cyclooxygenase lipoxygenase inhibitor, anti-inflammatory, cytotoxicity, diaryl imidazolone derivatives, molecular docking study and other aspects.Application In Synthesis of 2-(4-Methylbenzamido)acetic acid
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