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Design, synthesis and cytotoxic evaluation of β-aryl-α-dimethoxyphosphoryl-γ-lactamsCinar, SedaUnaleroglu, CananAk, AyşeGaripcan, BoraChemotherapeutic drugsIn vitro cytotoxic activityNitrovinyl arenesβ-Aryl-α-dimethoxyphosphoryl-γ-lactamsbeta aryl alpha dimethoxyphosphoryl gamma lactam derivativecytotoxic agentdimethyl [2 oxo 4 (thiophen 2 yl)pyrrolidin 3 yl]phosphonatedimethyl [4 (furan 2 yl) 2 oxopyrrolidin 3 yl]phosphonategamma lactam derivativemethyl 2 (dimethoxyphosphoryl) 3 (furan 2 yl) 4 nitrobutanoatemethyl 2 (dimethoxyphosphoryl) 4 nitro 3 (thiophen 2 yl) butanoateunclassified drugaddition reactionArticlecell viabilitycytotoxicitydrug designdrug screeningdrug synthesisglioblastoma cell linehumanhuman cellIC50in vitro studyL929 cell lineMCF-7 cell lineMichael additionneuroblastoma cell lineprostate cancer cell lineproton nuclear magnetic resonanceNew β-aryl-α-dimethoxyphosphoryl-γ-lactams 4a, b were designed and synthesized through the intra-molecular cyclization of 3a, b obtained from the addition reaction of methyl 2-(dimethoxyphosphoryl)acetate to (E)-2-(2-nitrovinyl)thiophene and (E)-2-(2-nitrovinyl)furan, respectively. The in vitro cytotoxicity of these compounds was evaluated against human breast cancer (MCF-7), rat glioblastoma (C6), prostate cancer (PC3), neuroblastoma (SHSY-5Y), and mouse fibroblast cell lines (L929). Dimethyl (4-(furan-2-yl)-2-oxopyrrolidin-3-yl)phosphonate (4b) was found to have cytotoxic activity towards MCF-7 and PC3 cell lines at the concentration values above 5 mM and 6 mM, respectively (IC50 values of MCF-7, 5.92 ± 1.86; PC3, 6.70 ± 2.10 mM). Dimethyl (2-oxo-4-(thiophen-2-yl)pyrrolidin-3-yl)phosphonate (4a) only decreased the viability of MCF-7 cells at 8 mM concentration (IC50 value of MCF-7 5.67 ± 1.70 in mM). In addition 4a, b had shown no significant cytotoxic effect on C6, SHSY-5Y and L929 cell lines. © 2017, Springer Science+Business Media New York.Birkhauser Boston2017Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/14933https://doi.org/10.1007/s00044-017-1816-y1054-2523enMedicinal Chemistry Researchinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/14933