YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity[1].
[1]. Yuan S, et al. Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors. J Med Chem. 2021;64(19):14895-14911.