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nm decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
we decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
mg decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
nn decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
nm decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
we decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
mg decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
nn decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
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Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance...
Published 2021“…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo[1,5-<i>a</i>]pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
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Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance...
Published 2021“…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo[1,5-<i>a</i>]pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
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Pharmacokinetic models and concentrations predictions of treatments considered.
Published 2021Subjects: -
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