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The Pharmaceutical Society of Korea (대한약학회)
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Preparation of N'-Substituted Anilino-N-Methyl-N-Nitorsoureas as Candidate Antitumor Agents

  • Kim, Jack-C (Department of Chemistry, College of Natural Sciences, Pusan National University) ;
  • Kim, Yeon-Gweon (Department of Chemistry, College of Natural Sciences, Pusan National University) ;
  • Min, Byoung-Tack (Department of Chemistry, College of Natural Sciences, Pusan National University) ;
  • Park, Jin-Il (Department of Chemistry, College of Natural Sciences, Pusan National University)
  • Published : 1994.12.01
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Abstract

Various N'-substituted anilino-N-methyl-N'-nitrosoureas(2a-n) were easily prepared from the reaction of substituted phenylhydraines $(3, 4-CH_3, {\;} 3-, {\;} 4-OCH_3, {\;} 3-, {\;} 4-F, {\;} 3, {\;} 4-Cl, {\;} 4-Br, {\;} 2-, {\;} 3-, {\;} 4-NO_2, 4-(NO_2)_2)$ with methyl isocyanate, followed by the nitrosation with 99% HCOOH and dry sodium lnitrite powder. Surprisingly, of these series of analogus, the anilino-nitrocosureas substituted with eletron-withdrawing nitro groups (2k-a) showed significantly low $ED_{30}$ values of $1.4-3.4 {\mu}g/ml.$ In addition, none of these copounds subtituted with electron-donating groups exhibited cytotoxicities.

Keywords

References

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