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. 2021 Feb 15;12:620874. doi: 10.3389/fphar.2021.620874

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Copyright © 2021 Yang, Wu, Wang, Teng, Lei, Lusvarghi, Ambudkar, Chen and Yang.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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Chemical structure of OTS964, and the cell viability-concentration curves for OTS964 and mitoxantrone in MDR cells mediated by ABCG2 and their counterparts in parental cells. (A) 2D view of OTS964 structure. (B) 3D view of OTS964 structure. OTS964 molecule is exhibited as colored sticks. Gray: carbon; white: hydrogen; red: oxygen; blue: nitrogen; yellow: sulfur. The cytotoxic activity of OTS964 in (C) S1-M1-80 and S1, (D) NCI-H460/MX20 and NCI-H460, and (E, F) ABCG2-transfected HEK293 cells (HEK293/ABCG2-482-R2, HEK293/ABCG2-482-G2, and HEK293/ABCG2-482-T7) and HEK293/pcDNA3.1 co-treated without/with Ko143. The cytotoxic activity of mitoxantrone in (G) S1-M1-80 and S1, (H) NCI-H460/MX20 and NCI-H460, and (I, J) ABCG2-transfected HEK293 cells (HEK293/ABCG2-482-R2, HEK293/ABCG2-482-G2, and HEK293/ABCG2-482-T7) and HEK293/pcDNA3.1 co-treated without/with Ko143. Ko143 served as a known ABCG2 inhibitor. Each dot is displayed as mean ± SD obtained from three experiments performed independently.