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[Design, synthesis, antibacterial and anti-cell proliferation activities of [1,2,4]triazino[3,4-h] [1,8]naphthyridine-8-one-7-carboxylic acid derivatives].
- Source :
-
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2015 Mar; Vol. 50 (3), pp. 332-6. - Publication Year :
- 2015
-
Abstract
- To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.
- Subjects :
- Animals
Anti-Bacterial Agents chemical synthesis
Antineoplastic Agents chemical synthesis
Carboxylic Acids
Carcinoma, Hepatocellular
Cell Line
Cell Proliferation
Escherichia coli drug effects
Fluoroquinolones chemical synthesis
HL-60 Cells
Humans
Leukemia L1210
Liver Neoplasms
Methicillin-Resistant Staphylococcus aureus drug effects
Mice
Naphthyridines
Triazines
Anti-Bacterial Agents chemistry
Antineoplastic Agents chemistry
Drug Design
Fluoroquinolones chemistry
Subjects
Details
- Language :
- Chinese
- ISSN :
- 0513-4870
- Volume :
- 50
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Yao xue xue bao = Acta pharmaceutica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 26118113