[The structural and functional analysis of the biological activity of acridine derivatives].

Abstract

The paper contains an analysis of research on designing drugs based on acridine derivatives. The discussed series of compounds is of essential value since acridines belong to the group of natural compounds with the pronounced antibacterial and anti-tumor activity. Improved chemical-synthesis techniques made it possible to synthesize both simple and complex compounds of the acridine series; they displayed a clear pharmacological activity as anti-proliferative, anti-tumor and antiparasitic preparations. The ability to induce interferons (INF), type 1, is an expected property of simple acridine derivatives. A variety of INF inducers, now used clinically, have been designed recently on the basis of the above compounds. The most well-known acridine derivatives, their pharmacological properties, action mechanisms and outlooks for practical application are described in the paper. The unique qualities of acridines are primarily attractive due to the possibility of using them for the purpose-oriented designing of drugs. Thus, acridines were used as a basis to create the specific regulatory HIV-1 elements, proliferation inhibitors of leukemia cells and new anti-tumor drugs. The elaboration of complexes of acridines derivatives combined with peptides intercalating specifically into the DNA big or small grooves is the most outstanding trend of acridines' research--it opens up prospects for using them in the synthesis of compounds regulating the gene expression.

• Authors: E G Deeva, Ia V Pavlovskaia, O I Kiselev, V I Kiselev, L B Piotrovskiĭ, F I Ershov
• Journal: Vestnik Rossiiskoi akademii meditsinskikh nauk (Vestn Ross Akad Med Nauk) Issue 2 Pg. 29-34 ( 2004) ISSN: 0869-6047 [Print] Russia (Federation)
• Vernacular Title: Strukturno-funktsional'nyĭ analiz biologicheskoĭ aktivnosti proizvodnykh akridina.
• PMID: 15101206 (Publication Type: English Abstract, Journal Article, Review)

Chemical References

• Acridines
• Anti-Infective Agents
• Antineoplastic Agents

Topics

• Acridines (chemical synthesis, chemistry, pharmacology)
• Anti-Infective Agents (chemical synthesis, chemistry, pharmacology)
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Combinatorial Chemistry Techniques
• Drug Design
• Drug Resistance, Multiple
• Humans
• Structure-Activity Relationship