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Synthesis and Evaluation of Topoisomerase I Inhibitors Possessing the 5,13-Dihydro-6H-benzo[6,7]indolo[3,2-c]quinolin-6-one Scaffold
http://hdl.handle.net/10069/39514
http://hdl.handle.net/10069/3951488ef67d9-e035-4da2-bb03-a3228416d535
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Het99_1032_SI.pdf (5.2 MB)
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Het99_1032.pdf (1.0 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2019-11-05 | |||||
タイトル | ||||||
タイトル | Synthesis and Evaluation of Topoisomerase I Inhibitors Possessing the 5,13-Dihydro-6H-benzo[6,7]indolo[3,2-c]quinolin-6-one Scaffold | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Fukuda, Tsutomu
× Fukuda, Tsutomu× Matsuoka, Fuyuki× Matsuo, Yuri× Yoshioka, Naoki× Onodera, Gen× Kimura, Masanari× Ishibashi, Fumito× Iwao, Masatomo |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Novel topoisomerase I inhibitors possessing the 5,13-dihydro- 6H-benzo[6,7]indolo[3,2-c]quinolin-6-one (BIQ) scaffold were designed and synthesized. This scaffold was constructed using sequential and regioselective functionalization of the pyrrole core through palladium-catalyzed cross-coupling, conventional electrophilic substitution, directed lithiation, and subsequent diphenylphosphoryl azide (DPPA)-mediated lactam ring construction. The obtained BIQs were evaluated for their topoisomerase I inhibitory activities and their antiproliferative activities in the panel of 39 human cancer cell lines established by the Japanese Foundation for Cancer Research (JFCR39). | |||||
書誌情報 |
HETEROCYCLES 巻 99, 号 2, p. 1032-1052, 発行日 2018-12-19 |
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出版者 | ||||||
出版者 | 日本複素環化学研究所 | |||||
出版者別言語 | ||||||
Japan Institute of Heterocyclic Chemistry | ||||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 03855414 | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.3987/COM-18-S(F)70 | |||||
権利 | ||||||
権利情報 | c 2019 The Japan Institute of Heterocyclic Chemistry | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | HETEROCYCLES, 99(2), pp.1032?1052; 2019 |