YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity

Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성

  • Baek Du-Jong (Department of Chemistry, College of Natural Sciences, Sangmyung University) ;
  • Ahn Jong-Woong (Division of Marine Environment & Bioscience, College of Ocean Science and Technology, Korea Maritime University) ;
  • Lee Chongock (Pharmaceutical Screening Laboratory, Korea Research Institute of Chemical Technology)
  • 백두종 (상명대학교 자연과학대학 화학과) ;
  • 안종웅 (한국해양대학교 해양환경 생명과학부) ;
  • 이정옥 (한국화학연구원 약리활성연구팀)
  • Published : 2005.02.01
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Abstract

Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

Keywords

References

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