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a decrease » _ decrease (Expand Search), _ decreased (Expand Search), _ decreases (Expand Search)
nm decrease » nn decrease (Expand Search), _ decrease (Expand Search), gy decreased (Expand Search)
we decrease » _ decrease (Expand Search), nn decrease (Expand Search), mean decrease (Expand Search)
n decrease » nn decrease (Expand Search), _ decrease (Expand Search), _ decreased (Expand Search)
a decrease » _ decrease (Expand Search), _ decreased (Expand Search), _ decreases (Expand Search)
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Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades
Published 2022“…Compound <b>4f</b> exhibited potent EGFR inhibitory activity with an IC<sub>50</sub> value of 61 nM compared to that of Tamoxifen (IC<sub>50</sub> value of 69 nM), with EGFR inhibition of 83 and 84%, respectively, at a concentration of 10 μM. …”
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Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades
Published 2022“…Compound <b>4f</b> exhibited potent EGFR inhibitory activity with an IC<sub>50</sub> value of 61 nM compared to that of Tamoxifen (IC<sub>50</sub> value of 69 nM), with EGFR inhibition of 83 and 84%, respectively, at a concentration of 10 μM. …”
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Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer
Published 2023“…Derivative <b>A11</b> directly binds to the insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) protein with a <i>K</i><sub>D</sub> value of 2.88 nM, which is about 23-fold more potent than CuB, leading to the decreased expression of downstream apoptosis- and cell cycle-related proteins. …”
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Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3‑Oxo-3,4-dihydro‑2<i>H</i>‑ben...
Published 2021“…Optimization of the left hand side afforded <b>4f</b> as a promising reversible MAGL inhibitor, which showed potent in vitro MAGL inhibitory activity (IC<sub>50</sub> 6.2 nM), good oral absorption, blood–brain barrier penetration, and significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3–10 mg/kg, po. in mice.…”
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Preclinical Evaluation of <sup>131</sup>I/<sup>18</sup>F‑Labeled Covalent Small-Molecule Inhibitors for STING Status Imaging
Published 2024“…The affinity and specificity of tracers were assessed through cell uptake and docking experiments, demonstrating that [<sup>131</sup>I]I-NFIP exhibited high specificity for STING, with a cell-based IC<sub>50</sub> value of 7.56 nM. …”
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Preclinical Evaluation of <sup>131</sup>I/<sup>18</sup>F‑Labeled Covalent Small-Molecule Inhibitors for STING Status Imaging
Published 2024“…The affinity and specificity of tracers were assessed through cell uptake and docking experiments, demonstrating that [<sup>131</sup>I]I-NFIP exhibited high specificity for STING, with a cell-based IC<sub>50</sub> value of 7.56 nM. …”
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