15 research outputs found
GSU Event Portal
GSU Event Portal focuses on providing an ease to people who wish to attend new events in a specific area of interest, where the events that are uploaded to the portal will be managed by the Event Organizers who are part of the portal. Portal provides free as well as paid events, so that people can choose events as per their interest. The portal provides Organizers the flexibility to create, manage, edit and remove events of any type and size. On the other side, Visitors can lookup events, they can save an event for their future interest and also pay for an event where applicable. The application provides a user-friendly interface so that the Organizers and the Visitors can get the benefits of the service provided by the event without any trouble. The application helps users to find an event they wish to attend with ease. They can browse events according to location, date and type. The main objective of the portal is advertising which helps the organizers to advertise their events and grab as much attention of the people to make their event more successful. This age is the age of technology and online advertising of event can help the organizers to attract more people in an easy way compared to paper advertisement. The people interested in an event, can even buy tickets of that event through this portal
A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches
Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic
Click-chemistry mediated synthesis of OTBN-1,2,3-Triazole derivatives exhibiting STK33 inhibition with diverse anti-cancer activities
There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer properties. To this end, a new series of 4′-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of bioactive compounds were designed and synthesized from diverse alkynes and N3-OTBN, using copper (II) acetate monohydrate in aqueous dimethylformamide at room temperature. Besides being highly cost-effective and significantly reducing synthesis, the reaction yielded 91–98 % of the target products without the need of any additional steps or chromatographic techniques. Two analogues exhibit promising anti-cancer biological activities. Analogue 4l shows highly specific cytostatic activity against lung cancer cells, while analogue 4k exhibits pan-cancer anti-growth activity. A kinase screen suggests compound 4k has single-digit micromolar activity against kinase STK33. High STK33 RNA expression correlates strongly with poorer patient outcomes in both adult and pediatric glioma. Compound 4k potently inhibits cell proliferation, invasion, and 3D neurosphere formation in primary patient-derived glioma cell lines. The observed anti-cancer activity is enhanced in combination with specific clinically relevant small molecule inhibitors. Herein we establish a novel biochemical kinase inhibitory function for click-chemistry-derived OTBN-1,2,3-triazole analogues and further report their anti-cancer activity in vitro for the first time
A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches
Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic
Click-chemistry mediated synthesis of OTBN-1,2,3-Triazole derivatives exhibiting STK33 inhibition with diverse anti-cancer activities
There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer properties. To this end, a new series of 4′-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of bioactive compounds were designed and synthesized from diverse alkynes and N3-OTBN, using copper (II) acetate monohydrate in aqueous dimethylformamide at room temperature. Besides being highly cost-effective and significantly reducing synthesis, the reaction yielded 91–98 % of the target products without the need of any additional steps or chromatographic techniques. Two analogues exhibit promising anti-cancer biological activities. Analogue 4l shows highly specific cytostatic activity against lung cancer cells, while analogue 4k exhibits pan-cancer anti-growth activity. A kinase screen suggests compound 4k has single-digit micromolar activity against kinase STK33. High STK33 RNA expression correlates strongly with poorer patient outcomes in both adult and pediatric glioma. Compound 4k potently inhibits cell proliferation, invasion, and 3D neurosphere formation in primary patient-derived glioma cell lines. The observed anti-cancer activity is enhanced in combination with specific clinically relevant small molecule inhibitors. Herein we establish a novel biochemical kinase inhibitory function for click-chemistry-derived OTBN-1,2,3-triazole analogues and further report their anti-cancer activity in vitro for the first time
Arthroscopic Anterior Cruciate Ligament Femoral Tunnel Visualization for Button Fixation
Arthroscopic reconstruction of the anterior cruciate ligament (ACL) remains one of the most commonly performed procedures in orthopaedic surgery. We describe a technique to visualize the button being advanced through the femoral tunnel using an arthroscope placed in the anteromedial portal. Looking into the femoral tunnel in line with the sutures, this technique allows the surgeon to directly visualize the femoral button as it traverses the femoral tunnel and confirms that it is engaged over the femoral cortex. Certain complications can arise, however, with the use of a suspensory fixation with a button on the femoral cortex. This method can decrease operative time and complication rates
Analysis of sex as a biological variable in cardiovascular research
For personalized medicine to achieve its full potential, inclusion of biological sex as a variable needs to become the norm in pre-clinical research practices (Woodward, 2019b). Consequences of not disaggregating biological sex (not reporting on study outcomes in male and females separately) include misdiagnosis of men and women differently who should have differing prognoses. Another concern is the prevalence of adverse drug effects that result from sex-specific differences (Kleefstra et al., 2019).
Cardiac diseases are a major health concern in which women are generally under-diagnosed and inappropriately treated for heart failure (Woodward, 2019a). Males are more likely to die from a cardiac event, and tend to be over-represented in clinical trials (Woodward, 2019a). However, factors like diabetes, smoking, and pregnancy put women at a higher risk for heart failure than men (Woodward, 2019b). Furthermore, having a male doctor may put females at a higher risk for mismanaging a cardiac disease and having a poor outcome (Woodward, 2019a). The field of cardiovascular research needs to substantially improve how pre-clinical and clinical studies are designed to provide more comprehensive analyses of biological sexes so we can better treat cardiovascular medical issues (Schiebinger and Klinge, 2013) and better understand disease mechanisms.
The main objective of this study is to evaluate the progress in reporting sex differences in mechanistic and pharmacological studies in biomedical research. In the last few decades several initiatives have been funded and installed for increasing the analysis of sex as a biological variable and how it alters risk analysis (Lee, 2018). As of 2015, it is federal policy to consider sex as a biological variable in NIH-funded Research (NOT-OD-15-102), including molecular functions and clinical data. Stem cells, tissues and animal models need to be annotated for their biological sex and analyzed for how this factors into the different phenotypes studied in the biomedical community. This study will compare whether basic or clinical cardiovascular research studies are more or less likely to report sex differences. Reporting the use of both biological sexes has increased over the past decade in several fields (Woitowich, Beery and Woodruff, 2020), however different fields have increased their reporting at different rates. We will determine whether biological sex reporting has increased in the field of cardiovascular research, and if so, whether it is increasing at a rate that is faster or slower compared to other biomedical research fields. Further, we will investigate how many articles include a separate analysis of sexes in their analyses, and, if so, whether they report statistically significant sex-related differences
2-Furanylmethyl <i>N</i>-(2-propenyl)carbamate
The overexpression of protein phosphatase 5 (PP5) has been correlated to tumor cell reproduction, making it a candidate for small molecule drug therapy. Prior work has focused on functionalized and decorated scaffolds that maximize contacts within and around the active site. The assembly and testing of cantharidin derivatives decorated with functionalized attachments has been our focus in order to affect the optimal binding of PP5. Condensation of 2-hydroxymethylfuran with allyl isocyanate meets the metrics of the rapid installment of functionality, as part of the core scaffold. Once condensed, cycloaddition followed by hydrogenation produces the desired derivative of norcantharidin in three synthetic steps
Angle Stable Nails Provide Improved Healing for a Complex Fracture Model in the Femur
Background Conventional nails are being used for an expanding range of fractures from simple to more complex. Angle stable designs are a relatively new innovation; however, it is unknown if they will improve healing for complex fractures. Questions/purposes When comparing traditional and angle stable nails to treat complex open canine femur fractures, the current study addressed the following questions: do the two constructs differ in (1) radiographic evidence of bone union across the cortices; (2) stability as determined by toggle (torsional motion with little accompanying torque) and angular deformation; (3) biomechanical properties, including stiffness in bending, axial compression, and torsional loading, and construct failure properties in torsion; and (4) degree of bone tissue mineralization? Methods Ten hounds with a 1-cm femoral defect and periosteal stripping were treated with a reamed titanium angle stable or nonangle stable nail after the creation of a long soft tissue wound. Before the study, the animals were randomly assigned to receive one of the nails and to be evaluated with biomechanical testing or histology. After euthanasia at 16 weeks, all operative femora were assessed radiographically. Histological or biomechanical evaluation was conducted of the operative bones with nails left in situ compared with the nonoperative contralateral femora. Results Radiographic and gross inspection demonstrated hypertrophic nonunion in all 10 animals treated with the nonangle stable nail, whereas six of 10 animals treated with the angle stable nail bridged at least one cortex (p = 0.023). The angle stable nail construct demonstrated no toggle in nine of 10 animals, whereas all control femora exhibited toggle. The angle stable nail demonstrated less angular deformation and toggle (p ≤ 0.005) and increased compressive stiffness (p = 0.001) compared with the conventional nonangle stable nail. Histology demonstrated more nonmineralized tissue in the limbs treated with the conventional nail (p = 0.005). Conclusions Angle stable nails that eliminate toggle lead to enhanced yet incomplete fracture healing in a complex canine fracture model. Clinical Relevance Care should be taken in tailoring the nail design features to the characteristics of the fracture and the patient
Alkoxy-functionalised dihydropyrimido[4,5-b]quinolinones enabling anti-proliferative and anti-invasive agents
In this communication, we explored the synthesis of novel alkoxy-functionalised dihydropyrimido[4,5-b]quinolinones using a microwave-assisted multicomponent reaction. All the synthesized molecules were screened for anti-proliferative and anti-invasive activity against glioblastoma cells. 5c shows the most potent anti-proliferative activity with a half maximal effective concentration of less than 3 μM against primary patient-derived glioblastoma cells. 5c effectively inhibited invasion and tumor growth of 3D primary glioma cultures in a basement membrane matrix. This suggests that the novel compounds could inhibit both the proliferation and invasive spread of glioma and they were selected for further study.</p