Discovery of (R)-2-(6-methoxynaphthalen-2-yl) butanoic Acid as a potent and selective aldo-keto reductase 1C3 inhibitor

…, LJ Marnett, TM Penning

Index: Liedtke, Andy J.; Adeniji, Adegoke O.; Chen, Mo; Byrns, Michael C.; Jin, Yi; Christianson, David W.; Marnett, Lawrence J.; Penning, Trevor M. Journal of Medicinal Chemistry, 2013 ,  vol. 56,  # 6  p. 2429 - 2446

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Abstract

Type 5 17β-hydroxysteroid dehydrogenase, aldo-keto reductase 1C3 (AKR1C3) converts Δ4- androstene-3, 17-dione and 5α-androstane-3, 17-dione to testosterone (T) and 5α- dihydrotestosterone, respectively, in castration resistant prostate cancer (CRPC). In CRPC, AKR1C3 is implicated in drug resistance, and enzalutamide drug resistance can be surmounted by indomethacin a potent inhibitor of AKR1C3. We examined a series of ...