Synthesis and in vitro antitumor activity of novel naphthyridinone derivatives
A series of naphthyridinone derivatives based on la（a precursor of Voreloxin） were designed and synthesized.Seven compounds having 〉70%inhibition against HL60 at 30 μmol/L were further evaluated for their in vitro antitumor activity by SRB assay.Results reveal that thiazol-2-yl and 3-aminomethyl-4-b...
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| Veröffentlicht in: | Chinese chemical letters 2017-02, Vol.28 (2), p.235-239 |
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| container_title | Chinese chemical letters |
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| creator | Jia, Xue-Dong Wang, Shuo Wang, Ming-Hua Liu, Ming-Liang Xia, Gui-Min Liu, Xiu-Jun Chai, Yun He, Hong-Wei |
| description | A series of naphthyridinone derivatives based on la（a precursor of Voreloxin） were designed and synthesized.Seven compounds having 〉70%inhibition against HL60 at 30 μmol/L were further evaluated for their in vitro antitumor activity by SRB assay.Results reveal that thiazol-2-yl and 3-aminomethyl-4-benzyloxyimino-3-methylpyrrolidin-l-yl groups are optimal at the N-1 and C-7positions of naphthyridinone core,respectively.10 j exhibits broad-spectrum activity（IC_（50）：〈0.5-6.25 μmol/L） against all of the tested cell lines including Etoposide- and/or la-resistant ones,and is 1.3-fold to 〉100-fold more potent than the two references against eight of these cell lines. |
| doi_str_mv | 10.1016/j.cclet.2016.07.024 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 1001-8417 |
| ispartof | Chinese chemical letters, 2017-02, Vol.28 (2), p.235-239 |
| issn | 1001-8417 1878-5964 |
| language | eng |
| recordid | cdi_osti_scitechconnect_1396344 |
| source | Elsevier ScienceDirect Journals; Alma/SFX Local Collection |
| subjects | Antitumor activity Naphthyridinones Synthesis Voreloxin |
| title | Synthesis and in vitro antitumor activity of novel naphthyridinone derivatives |
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