Hypoxia-selective antitumor agents. 15. Modification of rate of nitroreduction and extent of lysosomal uptake by polysubstitution of 4-(alkylamino)-5-nitroquinoline …
…, GJ Atwell, RF Anderson, P Wardman…
文献索引：Siim, Bronwyn G.; Atwell, Graham J.; Anderson, Robert F.; Wardman, Peter; Pullen, Susan M.; Wilson, William R.; Denny, William A. Journal of Medicinal Chemistry, 1997 , vol. 40, # 9 p. 1381 - 1390
Studies have shown that 4-(alkylamino)-5-nitroquinolines possess high selectivity (20-60- fold) for hypoxic tumor cells in vitro, but are not active as hypoxia-selective cytotoxins (HSCs) in vivo. The compounds show inadequate rates of extravascular diffusion, likely due both to sequestration of the bisbasic compounds into lysosomes and rapid nitroreduction. A further series of analogues, designed to counteract these limitations, has been synthesized and ...
