[Acridines as antitumor drugs]. / Akrydyny jako zwiazki aktywne przeciwnowotworowo.

Acridines belong to a group of polycyclic heteroaromatic compounds and exhibit a broad spectrum of biological activity including antiprotozoal, antibacterial, antiviral and antitumor activity. Acridine derivatives with antitumor activity have different mechanisms of action at the molecular level. The data obtained so far indicate that one of the main steps is the formation of physico-chemical complexes with DNA. Among acridine derivatives with anticancer activity we can distinguish five main classes of compounds: nitroacridines, 9-anilinoacridines, pyrazoloacridines, imidazoacridines, and triazoloacridines. Compounds from different classes differ both in mechanism of action and spectrum of antitumor activity.

[Thermodynamics aspects of interactions between small ligands and DNA]. / Termodynamiczne aspekty oddzialywania niskoczasteczkowych ligandów z DNA.

DNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measures changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other techniques measure changing in drug environment. With the increasing availability of sensitive microcalorimeters, particular interest has arisen in the thermodynamics of drug-DNA interaction. Using such methods permit direct determination of enthalpy changes associated with reactions. One experiment permits to obtain also binding constant, hence an almost complete thermodynamic profile can be established. This profile offers key insights into the molecular forces that drive complex formation and permit to estimate which kind of interaction are responsible of forming these complexes.