Search results for "Design"
showing 10 items of 5885 documents
Multi-disciplinary, Inter-disciplinary, Anti-disciplinary. Transition Knowledges in Design Education
2023
The environmental issues are recently proving to be the center and the connecting element of all the states of crisis, only apparently diversified (energy, political, migration); after the lucid forward-looking analysis of Maldonado in the 70s, the vision proposed in 2019 by the exhibition Broken Nature opens new spaces to the “design hope” activated by design, emphasizing the broad responsibility that the designer must take on contemporary challenges. The complex scenarios of the “transition” (environmental, cultural, productive) are also based on the ability of disciplinary encroachment and on the most radical forms of “anti-disciplinary” innovation, which in some cases opens to design fo…
Synthesis and biological evaluation of abietic acid derivatives
2009
A series of C18-oxygenated derivatives of abietic acid were synthesized and evaluated for their cytotoxic, antimycotic, and antiviral activities. In general, the introduction of an aldehyde group at C18 did improve the resultant bioactivity, while the presence of an acid or alcohol led to less active compounds.
A Novel Series of Acylhydrazones as Potential Anti-Candida Agents: Design, Synthesis, Biological Evaluation and In Silico Studies
2019
In the context of an increased incidence of invasive fungal diseases, there is an imperative need of new antifungal drugs with improved activity and safety profiles. A novel series of acylhydrazones bearing a 1,4-phenylene-bisthiazole scaffold was designed based on an analysis of structures known to possess anti-Candida activity obtained from a literature review. Nine final compounds were synthesized and evaluated in vitro for their inhibitory activity against various strains of Candida spp. The anti-Candida activity assay revealed that some of the new compounds are as active as fluconazole against most of the tested strains. A molecular docking study was conducted in order to evaluate the …
New antifungals selected by molecular topology.
1999
Abstract Molecular topology has been applied to find the new lead antimycotic compounds. Among the selected compounds stands out 3,3′-(4,4′ - Biphenylene)bis(2,5-diphenyl-2H-tetrazolium chloride), Benztropine mesylate and Dicyclopentamethylenethiuram disulphide, with minimum inhibitory concentrations between 1.6 and 2 μg / mL.
Recent advances in computational design of potent aromatase inhibitors: open-eye on endocrine-resistant breast cancers.
2019
Introduction: The vast majority of breast cancers (BC) are estrogen receptor positive (ER+). The most effective treatments to fight this BC type rely on estrogen deprivation therapy, by inhibiting the aromatase enzyme, which performs estrogen biosynthesis, or on blocking the estrogens signaling path via modulating/degrading the estrogen's specific nuclear receptor (estrogen receptor-?, ER?). While being effective at early disease stage, patients treated with aromatase inhibitors (AIs) may acquire resistance and often relapse after prolonged therapies. Areas covered: In this compendium, after an overview of the historical development of the AIs currently in clinical use, and of the computati…
Toward a Rational Design of Polyamine-Based Zinc-Chelating Agents for Cancer Therapies.
2020
In vitro viability assays against a representative panel of human cancer cell lines revealed that polyamines L1a and L5a displayed remarkable activity with IC50 values in the micromolar range. Preliminary research indicated that both compounds promoted G1 cell cycle arrest followed by cellular senescence and apoptosis. The induction of apoptotic cell death involved loss of mitochondrial outer membrane permeability and activation of caspases 3/7. Interestingly, L1a and L5a failed to activate cellular DNA damage response. The high intracellular zinc-chelating capacity of both compounds, deduced from the metal-specific Zinquin assay and ZnL2+ stability constant values in solution, strongly sup…
Negative-pressure cavitation extraction of cajaninstilbene acid and pinostrobin from pigeon pea [Cajanus cajan (L.) Millsp.] leaves and evaluation of…
2011
Abstract In this study, an efficient negative-pressure cavitation extraction (NPCE) technique was developed to extract cajaninstilbene acid (CSA) and pinostrobin (PI) from pigeon pea [Cajanus cajan (L.) Millsp.] leaves. The operating parameters were optimised using single-factor experiment and central composite design combined with response surface methodology. Well-fitting models for the extraction of CSA and PI were successfully established. From the economic perspective, the selected operating parameters were: extraction pressure −0.075 MPa, extraction temperature 45 °C, material size 40 mesh, ethanol concentration 80%, extraction time 30 min, liquid/solid ratio 30:1 and 4 extraction cyc…
Synthesis and evaluation of diverse thio avarol derivatives as potential UVB photoprotective candidates.
2007
Semisynthesis of 13 new thio avarol derivatives (4-16) and in vitro evaluation on the photodamage response induced by UVB irradiation are described. Their ability to inhibit NF-kappaB activation and TNF-alpha generation in HaCaT cells as well as their antioxidant capacity in human neutrophils has also been studied. Among them we have identified two monophenyl thio avarol derivatives (4-5) lacking cytotoxicity which can be considered promising UVB photoprotective agents through the potent inhibition of NF-kappaB activation with a mild antioxidant pharmacological profile.
Direct-acting antiviral agents and risk of hepatocellular carcinoma: is it still a clinical dilemma?
2019
Direct-acting antivirals (DAAs) revolutionised the treatment of chronic HCV-related disease achieving high rates of sustained virological response (SVR), also in more advanced patients, with a good safety profile and a proven positive effect on the reduction of risk of HCC occurrence. Nevertheless, patients with an history of successfully treated early HCC were initially excluded from pivotal trials. Although some initial retrospective studies, affected by several methodological issues, raised concerns regarding a possible harmful effect on the risk of HCC recurrence after antiviral therapy, more recent prospective studies and meta-analyses provided evidence that risk of HCC recurrence afte…
CardioPulse: developments in the treatment of aortic aneurysms in 2014
2015
Since the introduction of EndoVascular Aortic Repair (EVAR) for the treatment of abdominal aortic aneurysms (AAA) more than 20 years ago, the technique has evolved rapidly, from tubular grafts for fairly simple abdominal aortic anatomy, to bifurcated, fenestrated, branched, or parallel grafts for complex aortic aneurysms, no longer confined to the infrarenal abdominal aorta.