Isothiocyanates (ICTs) are a group of molecules that can be used for many different purposes, they exhibit anticancer, antimicrobial, antibiotic, and anti-inflammatory properties. The synthesis of isothiocyanates has been a focus of many researchers for nearly the past 100 years. One of the most common synthetic methods is to form a dithiocarbamate salt, either as the first step or in situ, and then treat the salt with a desulfurization agent to reach the isothiocyanate. There are many different desulfurization agents available. Among these, there are eleven in particular that will be discussed in this short review, namely thiophosgene, lead nitrate, ethyl chloroformate, hydrogen peroxide, triphosgene, iodine, cobalt, copper, sodium persulfate, claycop, and tosyl chloride. There are four additional particular methodologies that stand out from the literature available on this topic that will be covered, namely the production of isothiocyanates from hydroximoyl chlorides, via elemental sulfur, microwave-assisted synthesis, and through the tandem Staudinger/aza-Wittig reactions.1 Introduction1.1 Metabolism of Glucosinolates2 Synthesis of Isothiocyanates2.1 Isothiocyanates from the Decomposition of Dithiocarbamate Salts2.2 Isothiocyanates from Hydroximoyl Chlorides2.3 Isothiocyanates Produced via Elemental Sulfur2.4 Microwave-Assisted Synthesis of Isothiocyanates2.5 Isothiocyanates via the Tandem Staudinger/aza-Wittig Reactions3 Conclusion
A novel series of copper-activatable drugs intended for use against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillinresistant S. aureus (MRSA) were synthesized, characterized, and tested against the MSSA strain Newman and the MRSA Lac strain (a USA300 strain), respectively. These drugs feature an NNSN structural motif, which enables the binding of copper. In the absence of copper, no activity against MSSA and MRSA at realistic drug concentrations was observed. Although none of the novel drug candidates exhibits a stereocenter, sub-micromolar activities against SA Newman and micromolar activities against SA Lac were observed in the presence, but not in the absence, of bioavailable copper.Copper influx is a component of cellular response to bacterial infections, which is often described as nutritional immunity.
e16273 Background: There is a critical need to develop fast, reliable, and cost-effective methods for the detection of pancreatic cancer (PC) at the earliest stage to maximize the impact of treatment. To-date, early detection of PC is close to impossible due to the location of the pancreas and the absence of characteristic symptoms in early cancer stages. Methods: Our team of clinicians and scientists has established a fast and reliable nanobiosensor technology that comprises iron/iron oxide nanoparticles attached to a protease or arginase activatable FRET pair (tetrakis (4- carboxyphenyl) porphyrin (TCPP) /cyanine 5.5). Arginase and seven proteases (MMP1, 3, and 9, cathepsin B, and E, urokinase plasminogen activator, and neutrophil elastase) were identified using the Gene Expression Omnibus (GEO) web tool based on their different expression pattern in pancreatic cancer patients, pancreatitis and healthy control subjects. Protease/arginase activities were measured in serum after 1h of incubation. Based on this data, a novel engineering approach to improved early stage detection of pancreatic cancer is reported here. This study was funded by American Cancer Society Institutional Research Grant (IRG‐16‐194‐07), awarded to the University of Kansas Medical Center. Results: In our study, 159 patients were enrolled at KU Cancer Center from 2000-2019, 47 with metastatic PC, 36 with localized PC, 26 pancreatitis and 50 healthy controls using KUCC Biospecimen Repository. The problem of early stage detection of pancreatic cancer can be modeled as a multi-class classification problem. Conventional classification approaches provide at most 77% accuracy for the dataset under consideration. A new hierarchical decision structure with specific feature engineering at each step is introduced here to improve the performance of the classifier. The fundamental premise of this information fusion-based framework involves tailoring the statistically most significant features with appropriate weights to execute an efficient binary classification task at each hierarchical step. An overall accuracy of 95% was achieved for the detection of patients with early pancreatic cancer (see table). Conclusions: Because of the dire survival statistics of pancreatic cancer, detection at the earliest possible time by means of a liquid biopsy will offer the greatest benefit. Novel nanobiosensor based protease biomarkers achieved high accuracy in early detection of pancreatic cancers by applying hierarchical decision structure. Our results need validation in a larger cohort. Predicted true class considering the following combination of classification methods: Step1 – kNN*, step2 – kNN*, step3 – RFC* (Accuracy = 94.97%).[Table: see text]
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