- Synthesis and preliminary in vitro evaluation of antitumor nitrosoureido cholesterol derivatives
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A new class of chloroethyl nitrosourea analogues of cholesterol has been synthetized from the corresponding 7-amino and 7-aminoalkylcholesterol derivatives. Compounds III-V inhibited L1210 cell growth in culture much more effectively than N,N'-bis(2-cgloroethyl)-N'-nitrosourea (BCNU) after 48 h incubation. Stability and cytotoxic activity of these prodrugs are promising for brain tumor treatments and as lymphotropic vectors for tumor cells spreading along the lymphatic pathways.
- Elkihel,Gelin,Letourneux
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p. 190 - 194
(2007/10/02)
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- Novel procedure for the preparation of activated nitrosocarbamates
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The subject of the invention is a novel procedure for the preparation of the compounds of formula I: STR1 in which n varies in particular from 2 to 5 and R represents Cl, Br or F Z represents in particular hydrogen, characterized in that the halogenoformate of formula II: STR2 R and n having the meanings indicated above, Y representing a halogen, is made to react with NH2 CH2 CH2 Cl to form the compound of formula Ia: STR3 in which R has the meanings indicated above, and in that the compound Ia is treated directly with nitrosylsulfuric acid.
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- Activated N-Nitrosocarbamates for Regioselective Synthesis of N-Nitrosoureas
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A practical and convenient method for synthesizing antitumor compounds, N-alkyl-N-nitrosoureas, regioselectively nitrosated on the nitrogen atom bearing the alkyl group is proposed.N-Alkyl-N-nitrosocarbamates are interesting intermediates in these syntheses and yield, by reaction with amino compounds, the regioselectively nitrosated N-alkyl-N-nitrosoureas.As an interesting example, N,N'-biscystamine, a new attractive oncostatic derivative, has been prepared.The cytotoxic activity of these various compounds were tested on L1210 leukemia.
- Martinez, Jean,Oiry, Joel,Imbach, Jean Louis,Winternitz, Francois
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p. 178 - 182
(2007/10/02)
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