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KMID : 0370219970410060718
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Yakhak Hoeji
1997 Volume.41 No. 6 p.718 ~ p.723
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Synthesis and Cytotoxicity of 3-Carbamoyloxymethyl-1-azaanthraquinones
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이희순/Lee HS
최재영/홍승수/조정숙/김영호/Choi JY/Hong SS/Cho JS/Kim YH
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Abstract
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In the course of developing novel antitumor intercalating agents, we synthesized 3- carbamoyloxymethyl-azaanthraquinones 6-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of heteroatom incorporation into anthraquinone chromophore and the effect of the incorporation of the latent alkylating functionality. The derivatives were prepared by hetero Diels-Alder reaction as a key step followed by functionality of allylic 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 derivatives were 10 to lOO-fold less potent than doxorubicin against sensitive cell lines. However, they were marginally cross-resistant with doxorubicin against KB-V-1.
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