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http://dx.doi.org/10.12925/jkocs.2007.24.2.2

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

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)
Publication Information
Journal of the Korean Applied Science and Technology / v.24, no.2, 2007 , pp. 109-116 More about this Journal
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.
Keywords
[1,2,4]-Triazole derivatives; Anticancer activities; Cancer cell; SRB assay;
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