Journal of the Korean Applied Science and Technology (한국응용과학기술학회지)

The Korean Society of Applied Science and Technology (한국응용과학기술학회)
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Synthesis of [1,2,4]-Triazole Derivatives and Their Anticancer Activities

[1,2,4]-Triazole 유도체의 합성 및 항암활성

  • Lee, So-Ha (Life Sciences Research Division, Korea Institute of Science and Technology) ;
  • Kim, Jun-Suck (Department of Chemistry, Hankuk University of Foreign Studies) ;
  • Jeon, Jae-Ho (Department of Bio & Nano Chemistry, Kookmin University) ;
  • Lee, Sook-Ja (Department of Chemistry, Hankuk University of Foreign Studies)
  • 이소하 (한국과학기술연구원 생체과학연구본부) ;
  • 김준석 (한국외국어 대학교 화학과) ;
  • 전제호 (국민대학교 생명나노화학과) ;
  • 이숙자 (한국외국어 대학교 화학과)
  • Published : 2007.06.30
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Abstract

2-Chlorobenzoyl hydrazine refluxed with benzoyl isothiocyanate and phenyl isothiocyanate in ethanol for 3 hours to give benzamide derivative (1) and anilinederivative (2) on yield of 71%and 95%, respectively. Benzamide derivative (1) reacted with ethanolic sodium hydroxide on reflux to afford cyclization product (3), followed by general substitution reaction of two steps to give acetamide (5), and derivatived acetamides 7a-7k, while aniline derivative (2) reacted with ethanolic sodium hydroxide on reflux to afford another cyclization product (4). Thiol (4) reacted with N-phenyl chloroacetamide in the presence of potassim carbonate to give acetamide derivative (6). Compounds 1-7kwere evaluated for their growth inhibition against five cancer cell lines, including human lung carcinoma (A-549), human prostate cancer (DU145), human colon adenocarcinoma (HT-29), human malignant melanoma (SK-MEL-2) and human ovary malignant ascites (SK-OV-3) with sulforhodamine B (SRB) assay. All compounds (1-7k) showed low inhibition activities under 50% on 100M concentration.

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References

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