대한약학회:학술대회논문집 (Proceedings of the PSK Conference)
- 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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- Pages.351.2-351.2
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- 2002
Synthesis of Benzoquinoxalines
- Kwon, Nam-Koong (College of Pharmacy. Chungbuk National University) ;
- Lee, Hee-Soon (College of Pharmacy. Chungbuk National University)
- 발행 : 2002.10.01
초록
We have previously reported the synthesis and cytotoxic activities of a series of azaanthraquinone derivatives on the model of doxorubicin(Dox). Dox is known to intercalate into DNA and to inhibit topoisomerase II activity. But in the case of Quinone compounds like Dox. its use is limited because of systemic toxicities. primarily cardiotoxicity and myelosuppression. In this study. we describe the synthesis of benzoquinoxaline derivatives as DACA analogue. DACA has a neutral chromophore and acridine moiety and posions both topoisomerases I and ll with DNA intercalating activity. In order to delineate the SAR of benzoquinoxaline derivatives. an effcient sythetic rout to the target compounds without quinone group. Various attempted removal of quinone from benzoquinoxlinedione was unsuccessful. Diels-Alder rout applied for the synthesis of the target compounds will be discussed.
키워드