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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... by Shuai Wang (109515)

    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. …”
  20. 380

    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... by Shuai Wang (109515)

    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. …”