Monofunctional and Higher-Valent Platinum Anticancer Agents
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چکیده
منابع مشابه
Monofunctional and higher-valent platinum anticancer agents.
Platinum compounds represent one of the great success stories of metals in medicine. Following the serendipitous discovery of the anticancer activity of cisplatin by Rosenberg, a large number of cisplatin variants have been prepared and tested for their ability to kill cancer cells and inhibit tumor growth. These efforts continue today with increased realization that new strategies are needed t...
متن کاملNucleotide Binding Preference of the Monofunctional Platinum Anticancer-Agent Phenanthriplatin.
The monofunctional platinum anticancer agent phenanthriplatin generates covalent adducts with the purine bases guanine and adenine. Preferential nucleotide binding was investigated by using a polymerase stop assay and linear DNA amplification with a 163-base pair DNA double helix. Similarly to cisplatin, phenanthriplatin forms the majority of adducts at guanosine residues, but significant diffe...
متن کاملPhenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile.
Monofunctional platinum(II) complexes of general formula cis-[Pt(NH(3))(2)(N-heterocycle)Cl]Cl bind DNA at a single site, inducing little distortion in the double helix. Despite this behavior, these compounds display significant antitumor properties, with a different spectrum of activity than that of classic bifunctional cross-linking agents like cisplatin. To discover the most potent monofunct...
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A detailed study on the reaction mechanism of trans-EE and trans-EE/Met Pt-containing anticancer drugs was carried out in order to rationalize the experimental kinetic data concerning the whole process leading to DNA platination.
متن کاملFluorescent sensing of monofunctional platinum species.
We report here FDCPt1, a novel selective fluorescent sensor for monofunctional platinum species. In the presence of such species, FDCPt1 exhibits a 70-fold increase in fluorescence emission, and can be used to monitor the metabolism of Pt(II)-based complexes in colorectal cancer cells. This probe is therefore expected to be valuable in studying changes in Pt coordination and distribution during...
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ژورنال
عنوان ژورنال: Inorganic Chemistry
سال: 2013
ISSN: 0020-1669,1520-510X
DOI: 10.1021/ic400538c