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- Gazit, Aviv, et al.
(författare)
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Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit
- 2003
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Ingår i: Bioorganic & Medicinal Chemistry. - 0968-0896 .- 1464-3391. ; 11:9, s. 2007-2018
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Tidskriftsartikel (refereegranskat)abstract
- Here we report on novel quinoxalines as highly potent and selective inhibitors of the type III receptor tyrosine kinases PDGFR, FLT3, and KIT. These compounds, tricyclic quinoxalines, were generated in order to improve bioavailability over the highly hydrophobic bicyclic quinoxalines. Four of the highly active compounds were characterized in detail and are shown to inhibit PDGFR kinase activity of the isolated receptor as well as in intact cells in the sub-micromolar concentration range. We show that the most active inhibitor (compound 13, AGL 2043) is approximately 15-20 times more potent than its isomer (compound 14, AGL 2044). We therefore compared the three dimensional structures of the two compounds by X-ray crystallography. These compounds are also highly effective in blocking the kinase activity of FLT3, KIT, and the oncogenic protein Tel-PDGFR in intact cells. These compounds are potent inhibitors of the proliferation of pig heart smooth muscle cells. They fully arrest the growth of these cells and the effect is fully reversible. The chemical, biochemical and cellular properties of these compounds as well as the solubility properties make them suitable for development as anti-restenosis and anti-cancer agents.
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| 2. |
- Reb, Lennart K., et al.
(författare)
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Space‐ and Post‐Flight Characterizations of Perovskite and Organic Solar Cells
- 2023
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Ingår i: Solar RRL. - : Wiley. - 2367-198X. ; 7:9
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Tidskriftsartikel (refereegranskat)abstract
- Perovskite and organic solar cells are promising for space applications for enabling higher specific powers or alternative deployment systems. However, terrestrial tests can only mimic space conditions to a certain extent. Herein, a detailed analysis of irradiation-dependent photovoltaic parameters of perovskite and organic solar cells exposed to space conditions during a suborbital flight is presented. In orbital altitudes, perovskite and organic solar cells reach power-conversion efficiencies of more than 13% and 6%, respectively. Based on postflight grazing-incidence small-angle and wide-angle X-ray scattering, the active layer morphology and crystalline structure of the returned space solar cells are studied and compared to those of reference solar cells that stayed in an inert atmosphere. Minor changes in the active layer morphology are induced by the sole transport, without causing significant performance loss. For the space solar cells, morphological changes are attributed to the flight experiment that includes rocket launch, spaceflight, and reentry, as well as short-terrestrial environment exposure before and after launch. In contrast, no significant changes to the crystalline phase are observed. The notable performance during flight and high active layer stability, especially of perovskite solar cells, are promising results for further steps toward an orbital demonstration.
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