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KMID : 0043319830060020115
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Archives of Pharmacal Research
1983 Volume.6 No. 2 p.115 ~ p.121
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Synthesis and Primary Screening for Growth Inhibitors of L1210 Cells of Cholesteryl p-[3(2-chloroethyl)-3-nitrosoureido] phenylthioacetate
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Kim JC
Kim MS/Lee HK
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Abstract
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Cholesteryl p-[3-(2-chloroethyl)-3-nitrosoureido] phenylthioacetate (2) was synthesized:an intermediate, p-[3-(2-chloroethyl)-3-nitrosoureido] phenylthioacetic acid (1) is a congener of an antitumor chlorambucil which both the -CH2CH2- linkage and -N(CH2CH2Cl)2 group of chlorambucil molecule is doubly modified into the respective -S- linkage and -NH-CO-NNO-CH2CH2Cl group. The attackment of cholesterol moiety as a carrier group to p-[3-(2-chloroethyl)-3-nitrosoureido] phenylthioacetic acid was accomplished through the esterification of cholesterol with p-[3-(2-chloroethyl)-3-nitrosoureido] phenylthioacetyl chloride which was obtained from the treatment of p-[3-(2-chloroethyl)-3-nitrosoureido] phenylthioacetic acid with SOCl2. p-[3-(2-chloroethyl)ureido]-phenylthioacetic acid was nitrosated with NaNO2 in 98~100% HCOOH to give exclusively p-[3-(2-chloroethyl)-3-nitrosoureido]phenylthioacetic acid. Antitumor evaluation of compounds, 1 and 2 on L 1210 leukemia did show significant activity (ED40:1.14mcg/ml and 8.4mcg/ml, respectively). Further studies were subjected.
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KEYWORD
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