Fluorinated analogs of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea: an attempt to control metabolism

…, M Jarman, PL Coe, J Sleigh, JC Tatlow

Index: Foster, Allan B.; Jarman, Michael; Coe, Paul L.; Sleigh, John; Tatlow, J. Colin Journal of Medicinal Chemistry, 1980 , vol. 23, # 11 p. 1226 - 1229

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Citation Number: 6

Abstract

Notes solution, CCNU decomposes to give carbamylating and alkylating species. s However, rapid and extensive metabolism of CCNU occurs in vivo, presumably cytochrome P-450 mediated, to give various hydroxycyclohexyl derivatives (Scheme I). Seven such metabolites are possible theoretically, namely, the 1-hydroxy and the cis and trans forms of the 2-, 3-, and 4-hydroxy derivatives. The cis and trans forms of 2-, 3-, and 4-HO-CCNU ...