Cancer is a main reason for human morbidity and mortality globally. Screening and identifying new anticancer chemical substances is considered as a valid treatment for carcinoma. In our study on synthesis and search towards the development of potential anticancer agents, a series of thieno[2,3-d]pyrimidine derivatives were prepared from the functionalized iminophosphorane via aza-Wittig reaction. Their structures were confirmed by 1 H NMR, 13 C NMR, MS and elemental analysis. The in vitro antitumor activities of compounds were analyzed with CCK8 standard method. It revealed these thieno[2,3-d]pyrimi-dine derivatives were exhibited cytotoxicity against HepG2, HEp-2, and MCF-7 cell lines. The most potent compounds, 5 h and 5 j, were efficacious against HEp-2 cells with IC 50 1.8μmol/L and 0.8μmol/L, respectively. Meanwhile, 5 a, 5 d and 5 h showed broad spectrum of cytotoxicity for HepG2, Hep2 and MCF-7 three different cell lines with IC 50 range of 1.8-87.5μmol/L. Furthermore, we demonstrated that cytotoxicity of 5 j was due to the activation of caspase-9 involved apoptotic pathway, which is death receptor independent.
In an attempt to design and synthesize new heterocycles with improved their biological properties, some of fused tetracyclic benzo[4,5]furo[3,2‐d]pyrimidin‐ 4(3H)‐ones bearing 1,2,4‐triazole, 1,3,4‐thiadiazole, 1,2,4‐triazinanone, and oxazolidine systems have been prepared by the aza‐Wittig reactions from readily available starting material under mild conditions. The structure of synthesized compounds was elucidated by 1H NMR, 13C NMR, MS, IR, and elemental analysis.
Benzofuro[3,2- d]pyrimidine derivatives are prepared using aza-Wittig reactions of iminophosphoranes with n-butyl isocyanate at 40–50 °C to give carbodiimide intermediates, which are reacted with nitrogen-oxygen-containing nucleophiles to give 3-alkyl-2-amino (aryloxy/alkoxy)-benzofuro[3,2- d]pyrimidin-4(3 H)-ones in satisfactory yields in the presence of a catalytic amount of sodium ethoxide or K2CO3. The iminophosphorane also reacts directly with excess carbon disulfide, followed by n-propylamine; further reaction with alkyl halides or halogenated aliphatic esters in the presence of anhydrous K2CO3 produces the corresponding 2-alkylthio-3-n-propyl-benzofuro[3,2- d]pyrimidin-4(3 H)-ones in good yields. Their structures of the products are confirmed by 1H NMR, 13C NMR, mass spectrometry, infrared and elemental analysis.
Background: Infectious Meningitis/Encephalitis (M/E) is caused by pathogens. The FilmArray M/E panel can quickly detect 14 kinds of pathogens and facilitate diagnosis for patients with M/E. This study aimed to perform a evaluation of the sensitivity and specificity of the FilmArray M/E panel compared with classic method of diagnosing M/E.Methods: Relevant studies published before August 15, 2021, were identified by searching Web of Science, PubMed, Cochrane Library, and Embase, using keywords Meningitis, Encephalitis, and FilmArray M/E panel. After the initial screening, EndNoteX9 was used to manage the studies and extract data. The quality of the study was based mainly on the quality evaluation standard of diagnostic tests recommended by Quality Assessment of Diagnostic Accuracy Studies (QUADAS-2). Meta-DiSc 1.4 statistical software was used to determine the sensitivity, specificity, 95% confidence interval (CI), diagnostic odds ratio (DOR), positive likelihood ratios (PLR) and negative likelihood ratios (NLR) of each group of data, and summary receiver operating characteristic curve (SROC). All P values were two sided, and P <0.05 was considered statistically significant.Results: A total of 269 studies were retrieved, and 16 full-text studies were identified. The sensitivity of all the full-text studies was 0.93 (95% CI: 0.91–0.95) and the specificity 0.98 (95% CI: 0.98–0.98). Conclusions: Compared with the gold standard, the FilmArray M/E panel had a sensitivity of 0.93 and a specificity of 0.98 to 16 pathogens. Further studies are needed to determine whether the FilmArray M/E panel can be used as a clinical standard for the diagnosis of M/E.
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