Synthesis and evaluation of a series of 3, 5-disubstituted benzisoxazole-4, 7-diones. Potent radiosensitizers in vitro

…, CD Pinter, WE Elliott, JS Sebolt-Leopold

Index: Suto; Stier; Winters; Turner; Pinter; Elliott; Sebolt-Leopold Journal of Medicinal Chemistry, 1991 , vol. 34, # 11 p. 3290 - 3294

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Citation Number: 5

Abstract

A series of 3, 5-disubstituted-2, l-benzisoxazole-4, 7-diones was synthesized and evaluated as radiosensitizers both in vitro and in vivo. These compounds were designed as non-nitro electron-affinic agents in an effort to alleviate some of the toxicities seen with the 2- nitroimidazole radiosensitizers evaluated in the clinic. Several compounds in this series were potent radiosensitizers in vitro, with sensitizer enhancement ratios of 2.0-2.3 at ...