Current Topics in Medicinal Chemistry - Volume 11, Issue 21, 2011

The general concept of chemotherapy was introduced by Ehrlich about a century ago in which a systematic variation of structures and studies on the biological activity of antimicrobials resulted in the development of salvarsan. The concept has been followed by researchers all over the world and numerous compounds have been screened for other medicinal applications since Ehrlich's pioneering work, including many for their Read More

Over the past four decades, the search for improved platinum drugs based on the classical platinum(II)- diam(m)ine pharmacophore has yielded only a handful of successful candidates. New methodologies centred on platinum( IV) complexes, with better stability and expanded coordination spheres, offer the possibility of overcoming limitations inherent to platinum(II) drugs. In this review, novel strategies of targeting and killi Read More

The potential and limitations of the non classical metallodrugs with platinum as metal are discussed in this section, focusing not only in their design but in their mechanism of action and interaction with other biomolecules to introduce and encourage the readers on the potential of this field.

This review summarizes clinical and pre-clinical results on platinum anti-cancer drug formulations. A concise summary of the use of oxidation state to modulate cancer pharmacology is given for Pt(IV) complexes, distinct from the clinically used Pt(II) drugs. The chemistry of platinum drug formulation combines aspects of kinetics of active moiety release from nominally weak-binding ligands (bond cleavage from platinum-c Read More

Platinum-based drugs present one of the pillars of anticancer chemotherapy, and pharmaceuticals incorporating metals such as ruthenium, gallium, titanium and gold, some of which have already entered clinical trials, show promising features including activity against platinum-resistant tumors and/or reduced side-effects. The mode of action of these novel metallodrugs has only been partly elucidated, and even for estab Read More

Nowadays, gold compounds constitute a family of very promising experimental agents for cancer treatment. Indeed, several gold(I) and gold(III) compounds were shown to manifest outstanding antiproliferative properties in vitro against selected human tumor cell lines and some of them performed remarkably well even in tumor models in vivo. Notably, the peculiar chemical properties of the gold centre impart innovative Read More

In this review several types of interactions between metal ions and DNA are given, starting from basic binding to the use of metal complexes in cancer treatment and diagnostics. Metal cations help to neutralize the negative charge of DNA and thus enable the normal functions of DNA but many other interactions are also possible and are discussed in this paper. Various consequences of such interactions can be reversible ( Read More

Polynuclear compounds are a relatively new and successful approach in metal-based cancer chemotherapy as typified by the trinuclear Pt compound BBR3464 which was evaluated in clinical trials. In this review, we discuss newer developments of polynuclear ruthenium, osmium and gold complexes, focusing on their anticancer activity. The compounds presented are often supposed to exert their anticancer activity by Read More

The oxidative stress that is associated with the abnormal level of reactive oxygen species (ROS) is considered to be involved in the carcinogenesis process. The antioxidative defense system in the living organism regulates the toxic impact of ROS and there is strong evidence that the antioxidants prevent carcinogenesis. This review will focus on a novel approach to design synthetic metal-based antioxidants and to stud Read More