Synthetic methods for the preparation of ARQ 501 (β-lapachone) human blood metabolites

…, H Wu, E Volckova, XS Miao, SM Ali, M Tandon…

Index: Yang, Rui-Yang; Kizer, Darin; Wu, Hui; Volckova, Erika; Miao, Xiu-Sheng; Ali, Syed M.; Tandon, Manish; Savage, Ronald E.; Chan, Thomas C.K.; Ashwell, Mark A. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 10 p. 5635 - 5643

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Citation Number: 38

Abstract

ARQ 501 (3, 4-dihydro-2, 2-dimethyl-2H-naphthol [1, 2-b] pyran-5, 6-dione), a synthetic version of β-Lapachone, is a promising anti-cancer agent currently in multiple Phase II clinical trials. Promising anti-cancer activity was observed in Phase I and Phase II trials. Metabolism by red blood cells of drugs is an understudied area of research and the metabolites arising from oxidative ring opening (M2 and M3), decarbonylation/ring ...