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Inhibition of IL-2 production by novel small molecules using building blocks from reduced chalcones and a substituted proline

dc.contributor.authorDurán-Lara E.F.
dc.contributor.authorda Silva W.A.
dc.contributor.authorGuzmán L.
dc.contributor.authorCastro R.
dc.contributor.authorAndrade C.Z.
dc.contributor.authorSantos L.S.
dc.date.accessioned2020-09-02T22:16:45Z
dc.date.available2020-09-02T22:16:45Z
dc.date.issued2018
dc.identifier10.2174/1574885513666180209155439
dc.identifier.citation13, 2, 130-139
dc.identifier.issn15748855
dc.identifier.urihttps://hdl.handle.net/20.500.12728/4321
dc.descriptionBackground: Immunosuppressants are a class of drugs that can inhibit the immune response, mainly through the inhibition of IL-2 production, among other mechanisms. The most studied representatives of this class of therapeutic agents are Cyclosporin- A, FK506, and Rapamycin. Due to the structural complexity of these molecules, their chemical synthesis has been difficult and expensive. Objective: To synthesize novel small molecules that are structurally simple and that can be inhibitors of IL-2 production. These molecules are proposed to constitute new hypothetic immunosuppressant agents. Method: These small molecules were obtained through simple, cheap and efficient methods of well-known synthetic transformations. The molecules were synthetized in few steps through a highly convergent route and produced high yields. Results: Among the six compounds synthetized, compounds 4a1 and 4b2 showed interesting inhibitory activity. At higher concentration, compound 4a1 showed significant activity. However, the isomer 4a2 showed considerably less activity than 4a1, perhaps, for the high stereoselectivity ligand-receptor. Furthermore, the evaluation of the effect of novel molecules on the viability of mononuclear cells was carried out. The effect of the molecules proved to be innocuous. Conclusion: The data obtained from the inhibition of IL-2 production and low toxicity in mononuclear cells are promising for the development of future studies on these new hypothetic immunosuppressant agents. © 2018 Bentham Science Publishers.
dc.language.isoen
dc.publisherBentham Science Publishers B.V.
dc.subjectChalcones
dc.subjectIL-2 production
dc.subjectImmunosuppressants
dc.subjectN-substituted L-proline
dc.subjectSmall molecules
dc.subjectStereoselectivity
dc.subject1 benzyl 2 (1,5 diphenylpenta 2,4 dien 1 yl) pyrrolidine 1,2 dicarboxylate
dc.subject1 benzyl 2 [3 (4 chlorophenyl) 1 phenylallyl] pyrrolidine 1,2 dicarboxylate
dc.subject2 [3 (benzo[d][1,3]dioxol 5 yl) 1 phenylallyl] 1 benzyl pyrrolidine 1,2 dicarboxylate
dc.subjectchalcone derivative
dc.subjectimmunosuppressive agent
dc.subjectinterleukin 2
dc.subjectproline derivative
dc.subjectrapamycin
dc.subjectunclassified drug
dc.subjectArticle
dc.subjectbiological activity
dc.subjectcell viability
dc.subjectconcentration response
dc.subjectdrug receptor binding
dc.subjectdrug screening
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjectisomer
dc.subjectmononuclear cell
dc.subjectpriority journal
dc.subjectprotein synthesis inhibition
dc.subjectstereoselectivity
dc.subjectstructure analysis
dc.titleInhibition of IL-2 production by novel small molecules using building blocks from reduced chalcones and a substituted proline
dc.typeArticle


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