Figure 1.

Depiction of the most potent triple ABCB1, ABCC1, and ABCG2 inhibitors derived by HTS and synthesis approaches: 4-anilinopyrimidine 26 (1) as reported by Silbermann et al. in 2021;¹⁴ the tariquidar-related derivative 40 (2) as reported by Antoni et al. in 2021;²³ the amino aryl ester derivative (S)-9 (3) as reported by Teodori et al. in 2019;²⁶ pyrrolopyrimidine 55 (4) and indolopyrimidine 71 (5) as reported by Stefan et al. in 2017;¹⁷ the 2,4-substituted quinazoline derivative 52 (6) as reported by Krapf et al. in 2017;²⁸ 4-anilinoquinoline 29 (7) as reported by Krapf et al. in 2016;²⁹ thienopyridine 6r (8) as reported by Krauze et al. in 2014;³² benzoflavone 16 (9) as reported by Juvale et al. in 2013;³⁴ and the tetrahydroisoquinoline derivative MC18 (10) as reported by Colabufo et al. in 2008³⁹ and 2009.²¹