Sulfoxide-containing aromatic nitrogen mustards as hypoxia-directed bioreductive cytotoxins

…, Y Kim, E Wang, NZ Baturay, CH Kwon

Index: Sun; Botros; Su; Kim; Wang; Baturay; Kwon Journal of Medicinal Chemistry, 2000 , vol. 43, # 22 p. 4160 - 4168

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Citation Number: 81

Abstract

A series of diaryl and alkylaryl sulfoxide-containing nitrogen mustards were synthesized and evaluated for their hypoxia-selective cytotoxicity against V-79 cells in vitro as well as for their metabolism profiles with the rat S-9 fractions. In general, the diaryl sulfoxides (4, 5, and 7-9) showed much greater hypoxia selectivity (11-27-fold) than the alkylaryl sulfoxides (~ 3- fold)(1 and 3). The fused diphenyl sulfoxides (10 and 11), on the other hand, showed very ...