A strain-promoted alkyne-azide cycloaddition (SPAAC) reaction of a novel EpCAM aptamer-fluorescent conjugate for imaging of cancer cells

For the first time, a novel EpCAM aptamer (SYL3C)-DIBO-AF594 fluorescent conjugate was synthesised by bioorthogonal chemistry utilizing a strain promoted alkyne-azide cycloaddition (copper free click) reaction (SPAAC). The ligation efficiency of SPAAC was improved by freeze-thaw cycles. The obtained conjugate showed target specific binding and aided in the imaging of various EpCAM positive cancer cell lines like MCF7, MDAMB453, Weri-RB1 and PC3.

Characterizing university library use of social media: a case study of twitter and facebook from Australia

The work presented here characterise the engagement of one university library with two social media platforms popular with academic libraries. The collected data are analysed to identify the forms of Twitter and Facebook activity that engage library stakeholders in social media conversations. Associations were observed between: i) directed tweets from the library and mentions of the library by others on Twitter; and ii) comments from the library and comments from others on Facebook. Three broad classes of Twitter user interacting with the library were revealed: i) accounts strongly linked to the library with multiple to/from tweets; ii) those weakly linked to the library with, typically, a single tweet; and iii) those indirectly linked to the library through tweets mentioning the library and sent by other users. Two divergent forms of Facebook interaction with the library were highlighted: i) a library post generating a large sequence of comments, typically in response to a competition/challenge and ii) a library post with no comments, typically a photo post or a post inviting readers to click a link to find out more about an event/service. The work presented here is an initial investigation that provides useful insights, and offers a methodology for future research.

Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide.

A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, six 1,4-substituted-1,2,3-triazole derived bicalutamide mimics were synthesised in five steps and in isolated overall yields from 41% to 85%. Evaluation of these compounds for their anti-proliferative properties against androgen dependent (LNCaP) and independent (PC-3) cells showed promising IC50 values of 34-45 μM and 29-151 μM, respectively. The data suggest that the latter compounds may be an excellent starting point for the development of prostate cancer therapeutics for both androgen dependent and independent forms of this disease. Docking of these compounds (each enantiomer) in silico into the T877A mutated androgen receptor, as possessed by LNCaP cells, was also undertaken.

Novel immobilization of a quaternary ammonium moiety on keratin fibers for medical applications.

This paper introduces a new approach for immobilizing a quaternary ammonium moiety on a keratinous substrate for enhanced medical applications. The method involves the generation of thiols by controlled reduction of cystine disulfide bonds in the keratin, followed by reaction with [2-(acryloyloxy)ethyl]trimethylammonium chloride through thiol-ene click chemistry. The modified substrate was characterized with Raman and infrared spectroscopy, and assessed for its antibacterial efficacy and other performance changes. The results have demonstrated that the quaternary ammonium moiety has been effectively attached onto the keratin structure, and the resultant keratin substrate exhibits a multifunctional effect including antibacterial and antistatic properties, improved liquid moisture management property, improved dyeability and a non-leaching characteristic of the treated substrate.

Novel 1,4-substituted-1,2,3-triazoles as antitubercular agents

Tuberculosis (TB) remains a pressing unmet medical need, particularly with the emergence of multidrug-resistant and extensively drug-resistant tuberculosis. Here, a series of 1,4-substituted-1,2,3-triazoles have been synthesized and evaluated as potential antitubercular agents. These compounds were assembled via click chemistry in high crude purity and in moderate to high yield. Of the compounds tested, 12 compounds showed promising antitubercular activity with six possessing minimum inhibitory concentration (MIC) values <10 μg mL^-1, and total selectivity for Mycobacterium tuberculosis (Mtb) growth inhibition. A second set of 21 compounds bearing variations on ring C were synthesized and evaluated. This second library gave an additional six compounds displaying MIC values ≤10 μg mL^-1 and total selectivity for Mtb growth inhibition. These compounds serve as an excellent starting point for further development of antitubercular therapies.

A comparison of novel organoiridium(III) complexes and their ligands as a potential treatment for prostate cancer

A range of 1,4-substituted 2-pyridyl-N-phenyl triazoles were synthesised and evaluated for their antiproliferative properties against lymph node cancer of the prostate (LNCaP) and bone metastasis of prostate cancer (PC-3) cells. Excellent-to-low IC50 values were determined (5.6-250 μM), and a representative group of 4 ligands were then complexed to iridium(III) giving highly luminescent species. Re-evaluation of these compounds against both cell lines was then undertaken and improved potency (up to 72-fold) was observed, giving IC50 values of 0.36-11 μM for LNCaP and 0.85-5.9 μM for PC-3. Preliminary screens for in vivo toxicity were conducted using a zebrafish model showing a wide range of induced toxicity depending of the compound evaluated. Apoptosis and Caspase-3 levels were also determined and showed no statistical difference between some of the treated specimens and the controls. This study may identify novel therapeutic agents for advanced stage of prostate cancer in humans.

Rhodium(II) azavinyl carbenes and their recent application to organic synthesis

This highlight solely focusses on the synthetic applications of azavinyl rhodium(II) carbenes derived from N-sulfonyl triazoles. An overview of their use in intermolecular reactions to form a variety of heterocycles is examined, in addition to intramolecular annulations and rearrangements.

SUMLOW: Early design-stage sketching of UML diagrams on an e-whiteboard

Most visual diagramming tools provide point-and-click construction of computer-drawn diagram elements using a conventional desktop computer and mouse. SUMLOW is a unified modelling language (UML) diagramming tool that uses an electronic whiteboard (E-whiteboard) and sketching-based user interface to support collaborative software design. SUMLOW allows designers to sketch UML constructs, mixing different UML diagram elements, diagram annotations, and hand-drawn text. A key novelty of the tool is the preservation of hand-drawn diagrams and support for manipulation of these sketches using pen-based actions. Sketched diagrams can be automatically 'formalized' into computer-recognized and -drawn UML diagrams and then exported to a third party CASE tool for further extension and use. We describe the motivation for SUMLOW, illustrate the use of the tool to sketch various UML diagram types, describe its key architecture abstractions and implementation approaches, and report on two evaluations of the toolset. We hope that our experiences will be useful for others developing sketching-based design tools or those looking to leverage pen-based interfaces in software applications.