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[1,2,4]-Triazole 유도체의 합성 및 항암활성 KCI 등재

Synthesis of [1,2,4]-Triazole Derivatives and Their Anticancer Activities

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한국응용과학기술학회지 (The Korean Society of Applied Science and Technology)
한국응용과학기술학회(구 한국유화학회) (The Korean Society of Applied Science and Technology (KSAST))
초록

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.

저자
  • 이소하 | Lee, So-Ha
  • 김준석 | Kim, Jun-Suck
  • 전제호 | Jeon, Jae-Ho
  • 이숙자 | Lee, Sook-Ja