Synthesis of 5,9- and 5,8-Diaminoalkoxy Substituted Benzophenanthridinone Analogues as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors and Their Radiosensitizing Activity.

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Title: Synthesis of 5,9- and 5,8-Diaminoalkoxy Substituted Benzophenanthridinone Analogues as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors and Their Radiosensitizing Activity.
Authors: Hu DX; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; School of Pharmacy, Chengdu Medical College, Chengdu 610500, China., Qin C; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Guo LS; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Liu WY; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Liang ZQ; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Cao Y; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Yao CS; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China., Wei Y; Department of General Surgery (Colorectal Surgery), The Sixth Affiliated Hospital; Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University; Biomedical Innovation Center, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou 510655, China., Yue X; The First Affiliated Hospital, Jinan University, Guangzhou 510630, China., Mahmud MRA; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States., Agama K; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States., Wang H; Department of General Surgery (Colorectal Surgery), The Sixth Affiliated Hospital; Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University; Biomedical Innovation Center, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou 510655, China., Pommier Y; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States., An LK; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, Guangzhou 510006, China.
Source: Journal of medicinal chemistry [J Med Chem] 2025 May 08; Vol. 68 (9), pp. 9323-9340. Date of Electronic Publication: 2025 Apr 29.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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  Data: Synthesis of 5,9- and 5,8-Diaminoalkoxy Substituted Benzophenanthridinone Analogues as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors and Their Radiosensitizing Activity.
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  Data: <searchLink fieldCode="AU" term="%22Hu+DX%22">Hu DX</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; School of Pharmacy, Chengdu Medical College, Chengdu 610500, China.<br /><searchLink fieldCode="AU" term="%22Qin+C%22">Qin C</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Guo+LS%22">Guo LS</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Liu+WY%22">Liu WY</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Liang+ZQ%22">Liang ZQ</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Cao+Y%22">Cao Y</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Yao+CS%22">Yao CS</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.<br /><searchLink fieldCode="AU" term="%22Wei+Y%22">Wei Y</searchLink>; Department of General Surgery (Colorectal Surgery), The Sixth Affiliated Hospital; Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University; Biomedical Innovation Center, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou 510655, China.<br /><searchLink fieldCode="AU" term="%22Yue+X%22">Yue X</searchLink>; The First Affiliated Hospital, Jinan University, Guangzhou 510630, China.<br /><searchLink fieldCode="AU" term="%22Mahmud+MRA%22">Mahmud MRA</searchLink>; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States.<br /><searchLink fieldCode="AU" term="%22Agama+K%22">Agama K</searchLink>; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States.<br /><searchLink fieldCode="AU" term="%22Wang+H%22">Wang H</searchLink>; Department of General Surgery (Colorectal Surgery), The Sixth Affiliated Hospital; Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University; Biomedical Innovation Center, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou 510655, China.<br /><searchLink fieldCode="AU" term="%22Pommier+Y%22">Pommier Y</searchLink>; Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Institutes of Health, Bethesda, Maryland 20892, United States.<br /><searchLink fieldCode="AU" term="%22An+LK%22">An LK</searchLink>; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, Guangzhou 510006, China.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2025 May 08; Vol. 68 (9), pp. 9323-9340. <i>Date of Electronic Publication: </i>2025 Apr 29.
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        Value: 10.1021/acs.jmedchem.4c02951
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        Text: English
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      – TitleFull: Synthesis of 5,9- and 5,8-Diaminoalkoxy Substituted Benzophenanthridinone Analogues as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors and Their Radiosensitizing Activity.
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              Text: 2025 May 08
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