Anticancer Efficacy of Antibacterial Quinobenzothiazines
نویسندگان
چکیده
The antitumor potency of a series designed and prepared antibacterial quinobenzothiazines was evaluated against different types human cancer cell lines, such as glioblastoma SNB-19, lung adenocarcinoma A549 breast T47D, the activities compounds were compared to cisplatin doxorubicin. 9-Propoxy-5-methyl-12H-quino[3,4-b][1,4]benzo- thiazinium chloride (4a), 9-allyloxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium (4d) 11-benzyloxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium (4l) most active compounds; their IC50 values all three lines ranged from 5.3 9.3 µM. effective derivatives showed no cytotoxic effect up 100 µM on normal dermal fibroblasts (NHDFs). To explore structure–activity relationship, type/nature position substituents tetracyclic quinobenzothiazine system anticancer activity investigated. Additionally, receptor-dependent approach used specify mutual ligand–enzyme (bio)compositions that might be potentially valid for characteristics new derivatives. In particular, molecular docking procedure applied potent agents line T47D in order obtain comprehensive knowledge about aromatase–inhibitor binding mode. study revealed some regularities spatial atomic distribution nonbonding interactions (e.g., hydrophobic patterns) can observed molecules. surface electron-rich aromatic rings 4d 4l molecules could also contribute π–π stacking with protoporphyrin IX (HEM) well formation π–cation adjacent iron cofactor.
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ژورنال
عنوان ژورنال: Applied sciences
سال: 2023
ISSN: ['2076-3417']
DOI: https://doi.org/10.3390/app13052886