Title : Discovery of the Triazolo[1,5-a]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance.

Pub. Date : 2021 Nov 11

PMID : 34723530






4 Functional Relationships(s)
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1 Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo(1,5-a)pyrimidine derivative WS-898 as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
2 Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo(1,5-a)pyrimidine derivative WS-898 as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
3 WS-898 inhibited the efflux function of ABCB1, thus leading to decreased efflux and increased intracellular PTX concentration in SW620/Ad300 cells. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
4 The results suggest that WS-898 is a highly effective triazolo(1,5-a)pyrimidine-based ABCB1 inhibitor and shows promise in reversing ABCB1-mediated PTX resistance. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens