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A mild nitration of pyrrolo[2,1‐a]isoquinolines has been reached using sodium nitrite as nitro source in HFIP at ambient temperature. A variety of nitro‐bearing pyrrolo[2,1‐a]isoquinoline derivatives has been efficiently prepared in poor to quantitative yields (28–98 %). These products can be easily transformed to primary amines and amide by simple chemical reactions. Treatment of other nitrogen‐containing heterocycles such as pyrrolo[1,2‐a]quinoline and substituted indoles under this developed reaction system afforded nitro‐bearing N‐heterocycles in relatively lower yields (15–19 %). [ABSTRACT FROM AUTHOR]

We have developed an iron-catalyzed synthesis of pyrrolo[2,1- a ]isoquinoline derivatives with tetrahydroisoquinolines, arylacyl bromides, and nitroolefins. Highly functionalized pyrrolo[2,1- a ]isoquinolines can be obtained in moderate to good yields through a three-component N-alkylation/oxidative 1,3-dipolar cycloaddition/elimination/aromatization cascade. The obtained products in this study can be easily modified by easy chemical transformations to structurally complex molecules bearing privileged framework. [ABSTRACT FROM AUTHOR]

Purpose: Plasma markers that enable diagnosis in the early stage of lung cancer is not discovered. A liquid chromatography multiple reaction monitoring-mass spectrometry (LC-MRM-MS) assay for identifying potential early marker proteins for lung adenocarcinoma is developed., Experimental Design: LC-MRM-MS assay is used for measuring the level of 35 candidate peptides in plasma from 102 lung adenocarcinoma patients (including n = 50, 16, 24, and 12 in stage I, II, III, and IV, respectively.) and 84 healthy controls. Stable isotope labeled standard peptides are synthesized to accurately measure the amount of these proteins., Results: Seven proteins are able to distinguish stage I patients from controls. These proteins are combined in to a protein marker panel which improve the sensitivity to discriminate stage I patients from controls with cross-validated area under the curve = 0.76. Besides, it is found that low expression of eukaryotic initiation factor 4A-I and high expression of lumican show significantly poor prognosis in overall survival (p = 0.012 and 0.0074, respectively), which may be used as prognostic biomarkers for lung cancer., Conclusions and Clinical Relevance: Proteins highlighted here may be used for early detection of lung adenocarcinoma or therapeutics development after validation in a larger cohort., (© 2020 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)