약학회지 (YAKHAK HOEJI)

  • 제42권5호
  • /
  • Pages.507-512
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  • 1998
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  • 0377-9556(pISSN)
  • /
  • 2383-9457(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

4-카바모일옥시메틸-1-아자안트라퀴논 유도체들의 합성 및 세포독성

Synthesis and Cytotoxicity of 4-Carbamoyloxymethyl-1-azaanthraquinones

  • 발행 : 1998.10.01
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초록

In the course of developing novel antitumor intercalating agents. We synthesized 4-carbamoyloxymethyl-l-azaanthraquinones 7-12, incorporating the latent alkylating functi onality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354; liver and MCF7; breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resistant with doxorubicin against KB-V-1.

키워드

참고문헌

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