期刊
MOLECULAR AND CELLULAR BIOCHEMISTRY
卷 441, 期 1-2, 页码 151-163出版社
SPRINGER
DOI: 10.1007/s11010-017-3181-z
关键词
Organorhenium; Sulfonate; Carboxylate; MCF-7; MDA-MB-231; Breast cancers
类别
资金
- NCI
- NIH [T34 GM100831, G11HD038439]
- Nuclear Regulatory Commission [NRC-HQ-12-G-27-0086]
- Center for Biomolecular Therapeutics (CBT) at the University of Maryland, School of Medicine
Cisplatin and other metal-based drugs often display side effects and tumor resistance after prolonged use. Because rhenium-based anticancer complexes are often less toxic, a novel series of organorhenium complexes were synthesized of the types: XRe(CO)(3)Z (X = alpha-diimines and Z = p-toluenesulfonate, 1-naphthalenesulfonate, 2-naphthalenesulfonate, picolinate, nicotinate, aspirinate, naproxenate, flufenamate, ibuprofenate, mefenamate, tolfenamate, N-acetyl-tryptophanate), and their biological properties were examined. Specifically, in hormone-dependent MCF-7 and hormone-independent triple-negative MDA-MB-231 breast cancer cells, the p-toluenesulfonato, 1-naphthalenesulfonato, 2-naphthalenesulfonato, picolinato, nicotinato, acetylsalicylato, flufenamato, ibuprofenato, mefenamato, and N-acetyl-tryptophanato complexes were found to be far more potent than conventional drug cisplatin. DNA-binding studies were performed in each case via UV-Vis titrations, cyclic voltammetry, gel electrophoresis, and viscosity, which suggest DNA partial intercalation interaction, and the structure-activity relationship studies suggest that the anticancer activities increase with the increasing lipophilicities of the compounds, roughly consistent with their DNA-binding activities.
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