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Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.

He S, Chu X, Wu Y, Jiang J, Fang P, Chen Y, Liu Y, Qiu Z, Xiao Y, Li Z, Pan D, Zhang Q, Xie H, Xing S, Feng F, Liu W, Guo Q, Zhao L, Yang P, Sun H
J Med Chem 66 9537-9560 (2023)
Related entries: 7x3m, 8i0c

EuropePMC logo PMID: 37409679

Abstract

Aldo-keto reductase 1C3 (AKR1C3) is correlated with tumor development and chemotherapy resistance. The catalytic activity of the enzyme has been recognized as one of the important factors in inducing anthracycline (ANT) resistance in cancer cells. Inhibition of AKR1C3 activity may provide a promising approach to restore the chemosensitivity of ANT-resistant cancers. Herein, a series of biaryl-containing AKR1C3 inhibitors has been developed. The best analogue



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