Synthesis and evaluation of novel electrophilic nitrofuran carboxamides and carboxylates as radiosensitizers and bioreductively activated cytotoxins

…, MA Stephens, S Cole, MD Threadgill…

Index: Naylor, Matthew A.; Stephens, Miriam A.; Cole, Shirley; Threadgill, Michael D.; Stratford, Ian J.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2508 - 2513

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Citation Number: 19

Abstract

A series of 5-nitrofuran-2-and 3-carboxamides bearing alkylating side-chains has been synthesized and tested for their ability to radiosensitize selectively hypoxic Chinese hamster cells (V79) to the lethal effects of ionizing radiation and also for their ability to act directly and selectively as cytotoxic drugs on hypoxic V79 cells. The compounds were extremely efficient radiosensitizers of such cells in vitro and were more efficient than known nitroimidazoles ...