3-Trifluoromethyl-3-aryldiazirine photolabels with enhanced ambient light stability

2016 ◽  
Vol 52 (13) ◽  
pp. 2729-2732 ◽  
Author(s):  
Arun Babu Kumar ◽  
Jeremiah D. Tipton ◽  
Roman Manetsch

Ambient light stable 3-trifluoromethyl-3-aryldiazirine photolabels were designed, synthesized and evaluated. In addition to the enhancement to ambient light stability, the modified photolabels were equally efficient in labeling biological targets. The new photolabels also increase the aqueous solubility of the photoaffinity labels by several folds.


Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
G Lewin ◽  
A Maciuk ◽  
A Moncomble ◽  
JP Cornard


2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.



2020 ◽  
pp. 87-97
Author(s):  
Sourish Chatterjee ◽  
Biswanath Roy

In an office space, an LED-based lighting system allows you to perform the function of a data transmitter. This article discusses the cost-effective design and development of a data-enabled LED driver that can transmit data along with its receiving part. In addition, this paper clearly outlines the application of the proposed VLC system in an office environment where ambient light interference is a severe issue of concern. The result shows satisfactory lighting characteristics in general for this area in terms of average horizontal illuminance and illuminance uniformity. At the same time, to evaluate real-time and static communication performance, Arduino interfaced MATLAB Simulink model is developed, which shows good communication performance in terms of BER (10–7) even in presence of ambient light noise with 6 dB signal to interference plus noise ratio. Our designed system is also flexible to work as a standalone lighting system, whenever data communication is not required.



2010 ◽  
Vol E93-C (11) ◽  
pp. 1583-1589
Author(s):  
Fumirou MATSUKI ◽  
Kazuyuki HASHIMOTO ◽  
Keiichi SANO ◽  
Fu-Yuan HSUEH ◽  
Ramesh KAKKAD ◽  
...  


2019 ◽  
Vol E102.C (7) ◽  
pp. 558-564
Author(s):  
Takashi NAKAMURA ◽  
Masahiro TADA ◽  
Hiroyuki KIMURA


2017 ◽  
Vol 51 (4) ◽  
pp. 315-328
Author(s):  
Arturo Mendoza-Flores ◽  
Mario Villalobos ◽  
Teresa Pi-Puig ◽  
Nadia Valentina Martínez-Villegas


2020 ◽  
Author(s):  
Johannes Karges ◽  
Shi Kuang ◽  
Federica Maschietto ◽  
Olivier Blacque ◽  
Ilaria Ciofini ◽  
...  

<div>The use of photodynamic therapy (PDT) against cancer has received increasing attention overthe recent years. However, the application of the currently approved photosensitizers (PSs) is somehow limited by their poor aqueous solubility, aggregation, photobleaching and slow clearance from the body. To overcome these limitations, there is a need for the development of new classes of PSs with ruthenium(II) polypyridine complexes currently gaining momentum. However, these compounds generally lack significant absorption in the biological spectral window, limiting their application to treat deep-seated or large tumors. To overcome this drawback, ruthenium(II) polypyridine complexes designed in silico with (E,E’)-4,4´-bisstyryl 2,2´-bipyridine ligands showed impressive 1- and 2-Photon absorption up to a magnitude higher than the ones published so far. While non-toxic in the dark, these compounds were found phototoxic in various 2D monolayer cells, 3D multicellular tumor spheroids and be able to eradicate a multiresistant tumor inside a mouse model upon clinically relevant 1-Photon and 2 Photon excitation.</div>



2019 ◽  
Author(s):  
Sayan Mondal ◽  
Gary Tresadern ◽  
Jeremy Greenwood ◽  
Byungchan Kim ◽  
Joe Kaus ◽  
...  

<p>Optimizing the solubility of small molecules is important in a wide variety of contexts, including in drug discovery where the optimization of aqueous solubility is often crucial to achieve oral bioavailability. In such a context, solubility optimization cannot be successfully pursued by indiscriminate increases in polarity, which would likely reduce permeability and potency. Moreover, increasing polarity may not even improve solubility itself in many cases, if it stabilizes the solid-state form. Here we present a novel physics-based approach to predict the solubility of small molecules, that takes into account three-dimensional solid-state characteristics in addition to polarity. The calculated solubilities are in good agreement with experimental solubilities taken both from the literature as well as from several active pharmaceutical discovery projects. This computational approach enables strategies to optimize solubility by disrupting the three-dimensional solid-state packing of novel chemical matter, illustrated here for an active medicinal chemistry campaign.</p>





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