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Synthesis of Novel Allylthio Heterocyclo(or aryl)alkylaminopyridazines and Their Anticancer Activity against SK-Hep-1 Cells
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  • Synthesis of Novel Allylthio Heterocyclo(or aryl)alkylaminopyridazines and Their Anticancer Activity against SK-Hep-1 Cells
  • Synthesis of Novel Allylthio Heterocyclo(or aryl)alkylaminopyridazines and Their Anticancer Activity against SK-Hep-1 Cells
저자명
Lee. Myung-Sook,Kim. Eun-Sook,Moon. A-Ree,Park. Myung-Sook
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2009년|30권 1호|pp.83-91 (9 pages)
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대한화학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

To develop new anticancer agents, 3-allylthio-6-aminopyridazine derivatives were synthesized from maleic anhydrides or phthalic anhydrides by formation of a pyridazine nucleus, dichlorination, allylthiolation and amination. The pyridazine nuclei were obtained by condensing a hydrazine monohydrate with maleic anhydride. An allylthio group as a pharmacologically active group was introduced into one side of a pyridazine ring. Arylalkylamines with benzene or pyridine moieties or heterocycloalkylamines with heterocycle moieties such as morpholine, piperidine, or pyrrolidine were also introduced into the para-position of allylthio pyridazine. These new compounds showed antiproliferative activities against SK-Hep-1 human liver cancer cells in MTT assays. These compounds are thus promising candidates for chemotherapy of hepatocellular carcinomas. Two compounds, 20c and 22a, showed higher potencies for inhibiting growth of hepatocellular carcinoma cells than did K6 ($ID_50$=1.08 mM). This suggests the potential anticancer activity of these two compounds.