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• W3039878944 endingPage "112603" @default.
• W3039878944 startingPage "112603" @default.
• W3039878944 abstract "Abstract Cancer cells increase their glucose uptake and glycolytic activity to meet the high energy requirements of proliferation. Glucose transporters (GLUTs), which facilitate the transport of glucose and related hexoses across the cell membrane, play a vital role in tumor cell survival and are overexpressed in various cancers. GLUT1, the most overexpressed GLUT in many cancers, is emerging as a promising anti-cancer target. To develop GLUT1 inhibitors, we rationally designed, synthesized, structurally characterized, and biologically evaluated in-vitro and in-vivo a novel series of furyl-2-methylene thiazolidinediones (TZDs). Among 25 TZDs tested, F18 and F19 inhibited GLUT1 most potently (IC50 11.4 and 14.7 μM, respectively). F18 was equally selective for GLUT4 (IC50 6.8 μM), while F19 was specific for GLUT1 (IC50 152 μM in GLUT4). In-silico ligand docking studies showed that F18 interacted with conserved residues in GLUT1 and GLUT4, while F19 had slightly different interactions with the transporters. In in-vitro antiproliferative screening of leukemic/lymphoid cells, F18 was most lethal to CEM cells (CC50 of 1.7 μM). Flow cytometry analysis indicated that F18 arrested cell cycle growth in the subG0-G1 phase and lead to cell death due to necrosis and apoptosis. Western blot analysis exhibited alterations in cell signaling proteins, consistent with cell growth arrest and death. In-vivo xenograft study in a CEM model showed that F18 impaired tumor growth significantly." @default.
• W3039878944 created "2020-07-10" @default.
• W3039878944 creator A5010725738 @default.
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• W3039878944 date "2020-09-01" @default.
• W3039878944 modified "2023-10-15" @default.
• W3039878944 title "Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential" @default.
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• W3039878944 cites W1968963363 @default.
• W3039878944 cites W1970629182 @default.
• W3039878944 cites W1975701262 @default.
• W3039878944 cites W1976897494 @default.
• W3039878944 cites W1982166284 @default.
• W3039878944 cites W1982620914 @default.
• W3039878944 cites W1984495187 @default.
• W3039878944 cites W1985657228 @default.
• W3039878944 cites W1997715778 @default.
• W3039878944 cites W2003076573 @default.
• W3039878944 cites W2003910815 @default.
• W3039878944 cites W2004880100 @default.
• W3039878944 cites W2011505858 @default.
• W3039878944 cites W2014411539 @default.
• W3039878944 cites W2022131162 @default.
• W3039878944 cites W2027509142 @default.
• W3039878944 cites W2028897202 @default.
• W3039878944 cites W2029437336 @default.
• W3039878944 cites W2030324194 @default.
• W3039878944 cites W2032222317 @default.
• W3039878944 cites W2041321847 @default.
• W3039878944 cites W2043533862 @default.
• W3039878944 cites W2050545663 @default.
• W3039878944 cites W2052907531 @default.
• W3039878944 cites W2066033208 @default.
• W3039878944 cites W2072189471 @default.
• W3039878944 cites W2078972833 @default.
• W3039878944 cites W2085495751 @default.
• W3039878944 cites W2085663480 @default.
• W3039878944 cites W2094465598 @default.
• W3039878944 cites W2094907955 @default.
• W3039878944 cites W2097259163 @default.
• W3039878944 cites W2101604390 @default.
• W3039878944 cites W2104523208 @default.
• W3039878944 cites W2105649494 @default.
• W3039878944 cites W2107975811 @default.
• W3039878944 cites W2122113546 @default.
• W3039878944 cites W2123417241 @default.
• W3039878944 cites W2128730281 @default.
• W3039878944 cites W2135732933 @default.
• W3039878944 cites W2141129148 @default.
• W3039878944 cites W2162868196 @default.
• W3039878944 cites W2176791592 @default.
• W3039878944 cites W2223344044 @default.
• W3039878944 cites W2292751194 @default.
• W3039878944 cites W2336866153 @default.
• W3039878944 cites W2337937762 @default.
• W3039878944 cites W2418757312 @default.
• W3039878944 cites W2473040493 @default.
• W3039878944 cites W2473281810 @default.
• W3039878944 cites W2547960871 @default.
• W3039878944 cites W2593436234 @default.
• W3039878944 cites W2736351176 @default.
• W3039878944 cites W2737683399 @default.
• W3039878944 cites W2748609851 @default.
• W3039878944 cites W2760136945 @default.
• W3039878944 cites W2783084500 @default.
• W3039878944 cites W2801192506 @default.
• W3039878944 cites W2808391024 @default.
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• W3039878944 doi "https://doi.org/10.1016/j.ejmech.2020.112603" @default.
• W3039878944 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7451030" @default.
• W3039878944 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32634629" @default.
• W3039878944 hasPublicationYear "2020" @default.
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