908128-22-3Relevant academic research and scientific papers
Synthesis and cytotoxicity on human leukemia cells of furonaphthoquinones isolated from Tabebuia plants
Inagaki, Ryuta,Ninomiya, Masayuki,Tanaka, Kaori,Watanabe, Kunitomo,Koketsu, Mamoru
, p. 670 - 673 (2013/07/11)
Furonaphthoquinones are promising skeletons for anticancer drug molecules. In particular, methoxylated furonaphthoquinones are characteristic constituents of Tabebuia plants. In this research, we synthesized the furonaphthoquinones by effective one-pot ca
Synthetic methods for the preparation of ARQ 501 (β-Lapachone) human blood metabolites
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.
, p. 5635 - 5643 (2008/12/20)
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 contraction (M5), and decarbonylation/oxidation (M4 and M6) of ARQ 501 offer a unique opportunity to provide insight into these metabolic processes. Since these metabolites were not detected in in vitro incubations of ARQ 501 with liver microsomes and were structurally diverse, confirmation by chemical synthesis was considered essential. In this report, we disclose the synthetic routes employed and the characterization of the reference standards for these blood metabolites as well as additional postulated structures, which were not confirmed as metabolites.
