Site-specific incorporation of noncanonical amino acids (ncAAs) into proteins in eukaryotes has predominantly relied on the pyrrolysyl-tRNA synthetase/tRNA pair. However, access to additional easily engineered pairs is crucial for expanding the structural diversity of the ncAA toolbox in eukaryotes. The -derived leucyl-tRNA synthetase (EcLeuRS)/tRNA pair presents a particularly promising alternative.
View Article and Find Full Text PDFObjectives: This study aimed to establish an artificial intelligence (AI) system to classify vertical level differences between vocal folds during vocalization and to evaluate the accuracy of the classification.
Methods: We designed models with different depths between the right and left vocal folds using an excised canine larynx. Video files for the data set were obtained using a high-speed camera system and a color complementary metal oxide semiconductor camera with global shutter.
Bicyclo[1.1.0]butanes (BCBs), strained carbocycles comprising two fused cyclopropane rings, have become well-established building blocks in organic synthesis, medicinal chemistry, and chemical biology due to their diverse reactivity profile with radicals, nucleophiles, cations, and carbenes.
View Article and Find Full Text PDFTraditional radical-mediated ring-opening of bicyclo[1.1.0]butanes (BCBs) for cyclobutane synthesis suffers from poor diastereoselectivity.
View Article and Find Full Text PDFIntroduction: Automatic nuclear segmentation in digital microscopic tissue images can aid pathologists to extract high-quality features for nuclear morphometrics and other analyses. However, image segmentation is a challenging task in medical image processing and analysis. This study aimed to develop a deep learning-based method for nuclei segmentation of histological images for computational pathology.
View Article and Find Full Text PDFRecent advances in computer-aided detection via deep learning (DL) now allow for prostate cancer to be detected automatically and recognized with extremely high accuracy, much like other medical diagnoses and prognoses. However, researchers are still limited by the Gleason scoring system. The histopathological analysis involved in assigning the appropriate score is a rigorous, time-consuming manual process that is constrained by the quality of the material and the pathologist's level of expertise.
View Article and Find Full Text PDFThe novel coronavirus (COVID-19), which emerged as a pandemic, has engulfed so many lives and affected millions of people across the world since December 2019. Although this disease is under control nowadays, yet it is still affecting people in many countries. The traditional way of diagnosis is time taking, less efficient, and has a low rate of detection of this disease.
View Article and Find Full Text PDFA transition-metal-free, [2,3] sigmatropic rearrangement-annulation cascade of 2-substituted thio/amino acetonitriles with arynes allowing the synthesis of 2,4,5-trisubstituted oxazoles under mild conditions has been demonstrated. The key sulfur/nitrogen ylides were generated by the initial S/N arylation followed by proton transfer, which was followed by the selective [2,3] sigmatropic rearrangement involving the -CN moiety and a subsequent annulation to afford the desired products in reasonable yields.
View Article and Find Full Text PDFObjective: A primary brain tumor starts to grow from brain cells, and it occurs as a result of errors in the DNA of normal cells. Therefore, this study was carried out to analyze the two-dimensional (2D) texture, morphology, and statistical features of brain tumors and to perform a classification using artificial intelligence (AI) techniques.
Methods: AI techniques can help radiologists to diagnose primary brain tumors without using any invasive measurement techniques.
A facile synthesis of biologically important -aryl dithiocarbamates has been demonstrated by the aryne three-component coupling involving CS and aliphatic amines. This transition-metal-free and mild reaction is scalable and operates with good functional group compatibility. Preliminary mechanistic experiments, including density functional theory studies, are also provided.
View Article and Find Full Text PDFThe direct C2-functionalization of pyridines through a transition-metal-free protocol by using aryne multicomponent coupling is demonstrated. The reaction allowed a broad-scope synthesis of C2-substituted pyridine derivatives bearing the -CF group in good yields with α,α,α-trifluoroacetophenones as the third component. Activated keto esters could also be employed as the third component in this formal 1,2-di(hetero)arylation of ketones.
View Article and Find Full Text PDFAn oxa-[2,3] sigmatropic rearrangement involving arynes is reported featuring the umpolung of ketones, where the C═O bond polarity is reversed. The in situ-generated sulfur ylides from β-keto thioethers and arynes undergo efficient rearrangement allowing the facile and robust synthesis of functionalized enol ethers in high yields and excellent functional group compatibility. Preliminary mechanistic studies rule out the possibility of Pummerer-type rearrangement operating in this case.
View Article and Find Full Text PDFThe optimal diagnostic and treatment strategies for prostate cancer (PCa) are constantly changing. Given the importance of accurate diagnosis, texture analysis of stained prostate tissues is important for automatic PCa detection. We used artificial intelligence (AI) techniques to classify dual-channel tissue features extracted from Hematoxylin and Eosin (H&E) tissue images, respectively.
View Article and Find Full Text PDFAims: To prevent Alzheimer's disease (AD) from progressing to dementia, early prediction and classification of AD are important and they play a crucial role in medical image analysis.
Background: In this study, we employed a transfer learning technique to classify magnetic resonance (MR) images using a pre-trained convolutional neural network (CNN).
Objective: To address the early diagnosis of AD, we employed a computer-assisted technique, specifically the deep learning (DL) model, to detect AD.
The synthetic potential of thiophenols as a protic nucleophilic trigger in the transition-metal-free and Grignard-reagent-free three-component coupling involving arynes is demonstrated. Employing aldehydes as the third component, the reaction allowed the mild and broad scope synthesis of 2-arylthio benzyl alcohol derivatives in good yields. Moreover, selenophenol could be used as the nucleophilic trigger, and activated ketones could be used as the third component in this reaction.
View Article and Find Full Text PDFA mild and easy to perform multicomponent coupling involving phosphines, arynes generated from 2-(trimethylsilyl)aryl triflates, and CO allowing the transition-metal-free synthesis of zwitterionic phosphonium benzoates has been developed. The reaction proceeds via the generation of 1 : 1 zwitterionic intermediates from phosphines and arynes followed by the interception with CO to deliver the carboxylates in moderate to good yields instead of the anticipated benzooxaphosphol-3(1H)-ones.
View Article and Find Full Text PDFBackground: In this study, we used a convolutional neural network (CNN) to classify Alzheimer's disease (AD), mild cognitive impairment (MCI), and normal control (NC) subjects based on images of the hippocampus region extracted from magnetic resonance (MR) images of the brain.
Methods: The datasets used in this study were obtained from the Alzheimer's Disease Neuroimaging Initiative (ADNI). To segment the hippocampal region automatically, the patient brain MR images were matched to the International Consortium for Brain Mapping template (ICBM) using 3D-Slicer software.
Microscopic biopsy images are coloured in nature because pathologists use the haematoxylin and eosin chemical colour dyes for biopsy examinations. In this study, biopsy images are used for histological grading and the analysis of benign and malignant prostate tissues. The following PCa grades are analysed in the present study: benign, grade 3, grade 4, and grade 5.
View Article and Find Full Text PDFThe three-component coupling of tertiary amines, arynes, and aryl selenium bromide or diaryl diselenide as an electrophilic selenium source allowing the synthesis of 2-selanyl aniline derivatives is reported. This aminoselenation reaction of arynes installs a C-N and C-Se bond under mild conditions, and the products are formed in moderate to good yields. This reaction is compatible with various functional groups, and the preliminary studies on the mechanism of the reaction is also provided.
View Article and Find Full Text PDFAlthough azaoxyallyl cations are widely used as 1,3-dipoles for various cycloaddition reactions leading to nitrogen-containing heterocycles, their application in higher-order cycloaddition reaction remains scarce. Herein, we present the [8+3]-cycloaddition reaction of tropones with in situ generated azaoxyallyl cations allowing the one-step construction of cycloheptatriene-fused 1,4-oxazinones in moderate to good yields. This base-promoted new carbon-oxygen and carbon-nitrogen bond-forming reaction takes place under mild conditions in the absence of transition metal catalysts.
View Article and Find Full Text PDFThe synthetic utility of NaN as the azide component in the [3 + 2] annulation with arynes generated from 2-(trimethylsilyl)aryltriflates resulting in the transition-metal-free synthesis of -H and -aryl benzotriazoles has been demonstrated. Using CsF as the fluoride source in CHCN, the -H benzotriazoles are formed in high selectivity instead of the expected azidobenzene. Interestingly, -aryl benzotriazoles are formed using KF and THF as solvent in an open-flask reaction.
View Article and Find Full Text PDFThe synthetic potential of KI as the iodide source in aryne three-component coupling has been demonstrated using aldehydes as the third component. This mild and transition-metal-free coupling reaction allowed the straightforward synthesis of 2-iodobenzyl alcohols in moderate to good yields with good functional group compatibility. Moreover, KBr and KCl could be used as the nucleophilic trigger in this aryne multicomponent coupling (MCC) and N-methylisatin and CO could be used as the electrophilic third components.
View Article and Find Full Text PDFAn aryne induced transition-metal-free and mild Sommelet-Hauser rearrangement of tertiary benzylamines for the synthesis of α-aryl amino acid derivatives in moderate to good yields is presented. Unlike the conventional Sommelet-Hauser rearrangement of ammonium salts, the methodology developed herein requires neither harsh conditions nor strong bases. Moreover, a temperature dependent switchable selectivity for the Sommelet-Hauser and Stevens [1,2] rearrangements has been observed.
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