期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 57, 期 1, 页码 310-313出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201709968
关键词
antitumor agents; DNA structures; drug targeting; G-quadruplexes; platinum
资金
- CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico-Brasil)
- Royal Society-Newton Fellowships
- Leverhulme Trust [RPG 2014-225]
There has been increasing interest in the development of small molecules that can selectively bind to G-quadruplex DNA structures. The latter have been associated with a number of key biological processes and therefore are proposed to be potential targets for drug development. Herein, we report the first example of a reduction-activated G-quadruplex DNA binder. We show that a new octahedral platinum(IV)-salphen complex does not interact with DNA in aqueous media at pH7.4; however, upon addition of bioreductants such as ascorbic acid or glutathione, the compound is readily reduced to the corresponding square planar platinum(II) complex. In contrast to the parent platinum(IV) complex, the insitu generated platinum(II) complex has good affinity for G-quadruplex DNA.
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