Research on the Design of New Metal-Based Antitumor Drugs

Dear Colleagues,

The present issue of Pharmaceutics is devoted to the synthesis, structural characterization, and medical application potential of novel metal complexes designed to be antitumor agents. The main focus is on the innovative design of metal complexes with non-classical coordination polyhedra, engineered to provide extended and sustained antitumor effects and that can be tuned to overcome the drawbacks demonstrated by platinum drugs. In fact, metal compounds have been used for healing for a long time. Modern research on the application of metal complexes as drugs is associated with the remarkable but also “accidentally” created discovery of the healing properties of the seemingly simple coordination compound “nicknamed” cisplatin.

Approximately fifty years after its introduction into clinical practice, cisplatin and its structural analogs, generally recognized as antitumor drugs, are used “on the front line” in the treatment of various types of cancer and are included in various combination therapies. Despite their significant contribution to overcoming disease mortality, Pt(II)-drugs are not reproducibly effective against different tumor types, nor do they exhibit the same therapeutic effects in all patients. Recent intensive studies have shown that the search for a universal drug formula among cisplatin analogs has been replaced by the construction of new structures of chemotherapeutics that are effective in determining tumor types and targeting specific abnormalities of tumor cells.

Today, there are various approaches to designing the structures of new drugs, and for most of them, known mechanisms of action are the driving factors. Hence, the creation of effective anticancer drugs is usually guided by our knowledge of the mechanisms of their biotransformation and interactions in the biological environment. Further, the differences in the biochemistry of cancer cells can also be exploited to tune for specific action and to achieve selective activation and targeting. All these processes are a consequence of the chemical nature and the properties of the metal complexes. Thus, the specific structure of metal coordination compounds, which is characterized by a wide range of coordination numbers, attractive stereochemistry, structural diversity, different available redox states, the opportunity to “tune” the thermodynamic behavior and control the kinetics of ligand substitution reactions, as well as include additional organic drugs or targeting agents in the inner coordination sphere, etc., determine their enormous and underutilized potential in the treatment of cancer. Analyzing all of this, it can be concluded that efforts should be directed towards building a suitable coordination polyhedron with a proper selection of metal ions in suitable oxidation states as well as body-acceptable ligands to achieve a medicinal formula that suits all important requirements, such as a soluble form of the prodrug, presence of an inactivated form in the bloodstream, selective cellular uptake, activation of the drug in tumor cells, appropriate damage to tumor cells, etc.

We look forward to receiving your contributions which share new ideas and achievements in this important and rapidly developing field.

Dr. Galina G. Gencheva
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

• metal-based antitumor drugs
• transition metal complexes
• synthesis and physicochemical properties
• structural diversity and characterization
• antiproliferative effects
• mechanisms of cytotoxicity and common toxicity