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- W2600158104 abstract "We designed new hypoxia-activated prodrugs by conjugating (1-methyl-2-nitro-1H-imidazol-5-yl)methanol with 7-ethyl-10-hydroxy camptothecin (SN-38). Initially, we improved the method of multi-gram scale synthesis of (1-methyl-2-nitro-1H-imidazol-5-yl)methanol, which increased the yield to 42% compared to 8% by the original synthesis method. The improved method was used to synthesize evofosfamide (TH-302) and hypoxia-activated prodrugs of SN-38. Two different linkages between (1-methyl-2-nitro-1H-imidazol-5-yl)methanol and SN-38 were evaluated that afforded different hypoxia-selectivity and toxicity. Compound 16 (IOS), containing an ether linkage, was considered to be a promising hypoxia-selective antitumor agent." @default.
- W2600158104 created "2017-04-07" @default.
- W2600158104 creator A5008889596 @default.
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- W2600158104 date "2017-05-01" @default.
- W2600158104 modified "2023-09-27" @default.
- W2600158104 title "Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38" @default.
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- W2600158104 doi "https://doi.org/10.1016/j.ejmech.2017.03.040" @default.
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