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KMID : 0370219980420050507
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Yakhak Hoeji
1998 Volume.42 No. 5 p.507 ~ p.512
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Synthesis and Cytotoxicity of 4-Carbamoyloxymethyl-1-azaanthraquinones
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이희순/Lee HS
이승일/홍승수/조정숙/김영호/Lee SI/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 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.
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KEYWORD
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