THE EFFECT OF DIFFERENT METHODS OF SYNTHESIS ON THE TOXICITY AND EFFICIENCY OF NEW BIOLOGICALLY ACTIVE COMPOUNDS BASED ON THIENOPYRIMIDINES
DOI:
https://doi.org/10.32782/pcsd-2024-4-3Keywords:
bioactivity, synthesis of compounds, pharmacological action, chemical modification, cytotoxicity, anticancer activityAbstract
The second most common fatal disease in the world is cancer, the development of which is mediated by various physiological mechanisms, so the scientific approach to the synthesis of biologically active compounds for the treatment of cancer includes the understanding of new, specific biological targets and their correlation with this disease. In this aspect, thienopyridines and purine bioisosteres, which have a wide range of biological activities, including anticancer, are of interest. Therefore, this study aims to evaluate new approaches to synthesising thienopyridines and their influence on new compounds’ biological activity and toxicity. For this purpose, a theoretical study with elements of a scientific literature review was conducted using the PRISMA criterion. The scientific novelty of the work is to summarise the available heterogeneous data on the influence of the structure of synthesised thienopyridines on their activity and the known explanations of possible mechanisms of such influence. The study showed that the most attractive from the scientific point of view is the thieno[2,3-d]pyrimidine backbone, which is further modified by synthesising tricyclic structures, ‘grafting’ substituents of more complex structure to thienopyridine backbones, which in turn can be substituted, and creating hybrid molecules, for example, conjugates, each fragment of which has its biological activity. Moreover, cytotoxicity and antiproliferative activity are influenced by the type of a particular substituent, its ability to be an electron donor or acceptor, a combination of dissimilar substituents, as one substituent can reduce the activity of another, and the substitution site. Scientific studies show that substitution with dissimilar substituents in the same position can produce different cytotoxic effects and biological activity. Developing biologically active compounds based on thienopyridines for cancer treatment and new synthesis methods requires a serious interdisciplinary approach involving specialists in organic synthesis, organic molecule design, biology and pharmacology.
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