6-Substituted 6H-dibenzo[c,h][2,6]naphthyridin-5-ones: Reversed lactam analogues of ARC-111 with potent topoisomerase I-targeting activity and cytotoxicity

Shejin Zhu; Alexander L. Ruchelman; Nai Zhou; Angela Liu; Leroy-Fong Liu; Edmond J. LaVoie

doi:10.1016/j.bmc.2005.12.028

6-Substituted 6H-dibenzo[c,h][2,6]naphthyridin-5-ones: Reversed lactam analogues of ARC-111 with potent topoisomerase I-targeting activity and cytotoxicity

Shejin Zhu, Alexander L. Ruchelman, Nai Zhou, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

研究成果: 雜誌貢獻 › 文章 › 同行評審

23 引文斯高帕斯（Scopus）

摘要

6-Substituted 8,9-dimethoxy-2,3-methylenedioxy-6H-dibenzo[c,h][2,6] naphthyridin-5-ones were synthesized and evaluated for topoisomerase I-targeting activity and cytotoxicity. Several of these reversed lactam analogues of ARC-111 exhibited exceptional cytotoxicity with IC₅₀ values ranging from 0.5 to 3.0 nM. In contrast to topotecan, no resistance was observed with several of these reversed lactam analogues in tumor cell lines that overexpressed the efflux transporters MDR1 or BCRP.

原文	英語
頁（從 - 到）	3131-3143
頁數	13
期刊	Bioorganic and Medicinal Chemistry
卷	14
發行號	9
DOIs	https://doi.org/10.1016/j.bmc.2005.12.028
出版狀態	已發佈 - 五月 1 2006
對外發佈	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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6-Substituted 6H-dibenzo[c,h][2,6]naphthyridin-5-ones : Reversed lactam analogues of ARC-111 with potent topoisomerase I-targeting activity and cytotoxicity. / Zhu, Shejin; Ruchelman, Alexander L.; Zhou, Nai; Liu, Angela; Liu, Leroy-Fong; LaVoie, Edmond J.

於: Bioorganic and Medicinal Chemistry, 卷 14, 編號 9, 01.05.2006, p. 3131-3143.

研究成果: 雜誌貢獻 › 文章 › 同行評審

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abstract = "6-Substituted 8,9-dimethoxy-2,3-methylenedioxy-6H-dibenzo[c,h][2,6] naphthyridin-5-ones were synthesized and evaluated for topoisomerase I-targeting activity and cytotoxicity. Several of these reversed lactam analogues of ARC-111 exhibited exceptional cytotoxicity with IC50 values ranging from 0.5 to 3.0 nM. In contrast to topotecan, no resistance was observed with several of these reversed lactam analogues in tumor cell lines that overexpressed the efflux transporters MDR1 or BCRP.",

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AU - Liu, Leroy-Fong

AU - LaVoie, Edmond J.

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