Browsing by Subject "Small molecules"

Now showing 1 - 3 of 3

Open Access
Application of the Ugi reaction with multiple amino acid-derived components: Synthesis and conformational evaluation of piperazine-based minimalist peptidomimetics
(Royal Society of Chemistry, 2015) Stucchi, M.; Cairati, S.; Cetin-Atalay, R.; Christodoulou, M.S.; Grazioso G.; Pescitelli G.; Silvani, A.; Yildirim, D.C.; Lesma G.
The concurrent employment of α-amino acid-derived chiral components such as aldehydes and α-isocyanoacetates, in a sequential Ugi reaction/cyclization two-step strategy, opens the door to the synthesis of three structurally distinct piperazine-based scaffolds, characterized by the presence of l-Ala and/or l-Phe-derived side chains and bearing appropriate functionalities to be easily applied in peptide chemistry. By means of computational studies, these scaffolds have been demonstrated to act as minimalist peptidomimetics, able to mimic a well defined range of peptide secondary structures and therefore potentially useful for the synthesis of small-molecule PPI modulators. Preliminary biological evaluation of two different resistant hepatocellular carcinoma cellular lines, for which differentiation versus resistance ability seem to be strongly correlated with well defined types of PPIs, has revealed a promising antiproliferative activity for selected compounds. © The Royal Society of Chemistry 2015.
Open Access
Influence of gold-silica nanoparticles on the performance of small-molecule bulk heterojunction solar cells
(Elsevier BV * North-Holland, 2015) Xu, X.; Kyaw, A. K. K.; Peng, B.; Xiong, Q.; Demir, Hilmi Volkan; Wang Y.; Wong, T. K. S.; Sun, X. W.
Light trapping by gold (Au)-silica nanospheres and nanorods embedded in the active layer of small-molecule (SM) organic solar cell has been systematically compared. Nanorod significantly outperforms nanosphere because of more light scattering and higher quality factor for localized surface plasmon resonance (LSPR) triggered by nanorods. The optimum concentration of nanorod was characterized by charge carrier transport and morphology of the active layers. At optimum nanorod concentration, almost no change in the morphology of the active layer reveals that LSPR and scattering effects rather than the morphology are mainly responsible for the enhanced power conversion efficiency. In addition, the preliminary lifetime studies of the SM solar cells with and without Au-silica nanorods were conducted by measuring the current density-voltage characteristics over 20 days. The results show that plasmonic device with nanorods has no adverse impact on the device stability
Open Access
Site-specific fluorescence polarization for studying the disaggregation of α-synuclein fibrils by small molecules
(American Chemical Society, 2017) Haney, C. M.; Cleveland, C. L.; Wissner, R. F.; Owei, L.; Robustelli, J.; Daniels, M. J.; Canyurt, M.; Rodriguez, P.; Ischiropoulos, H.; Baumgart, T.; Petersson, E. J.
Fibrillar aggregates of the protein α-synuclein (αS) are one of the hallmarks of Parkinson’s disease. Here, we show that measuring the fluorescence polarization (FP) of labels at several sites on αS allows one to monitor changes in the local dynamics of the protein after binding to micelles or vesicles, and during fibril formation. Most significantly, these site-specific FP measurements provide insight into structural remodeling of αS fibrils by small molecules and have the potential for use in moderate-throughput screens to identify small molecules that could be used to treat Parkinson’s disease. © 2016 American Chemical Society.