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KMID : 0043319980210010073
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Archives of Pharmacal Research
1998 Volume.21 No. 1 p.73 ~ p.75
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Synthesis and In vitro Evaluation of 4-Substituted-1-azaanthraquinones
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Lee Hee-Soon
Hong Seong-Soo
Choi Jae-Young
Cho Jung-Sook
Kim Young-Ho
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Abstract
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In summary, six 4-substituted-1-azzanthraquinones were designed and synthesized using hetero Diels-Alder reaction as a key step. Although a great number of reaction conditions for benzylic bromination were examined, this step need to be improved for the efficient synthesis of the related analogues. 4-Bromomethyl-1-azzanthraquinone 6 may have potential for the treatment of tumors resistant to the doxorubicin. The compounds 9 and 10 containing the latent alkylating functionality may need further in depth biological evaluation. Work is in progress to design, synthesize, and evaluate additional compounds in this and related systems.
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KEYWORD
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Antitumor agents, azaanthraquinone, bio-reductive activation, cytotoxic activity, hetero Diels-Alder reaction, doxorubicin, and mitoxantrone
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