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The role of benzoazoles as a privileged scaffolds in development of novel lead compounds with antitumor potential

One of the main trends in medical chemistry along with the rational design and development of new and more effective biologically active compounds is the development of modern strategies for their synthesis. Heterocyclic nuclei offer a huge area for new lead molecules for drug discovery and for generation of activity relationships with biological targets for enhance pharmacological effects. In general, heterocyclic compounds containing a nitrogen atom are a significant source of pharmacologically active compounds. Therefore, in the last 15 years the concept of privileged scaffolds was introduced into medicinal chemistry. Such structures exhibit drug-like properties and are selected as chemical entities in the preparation of compound libraries with potential biological activity [1, 2]. Privileged scaffolds include purine and purinomimetics such as benzothiazole, benzimidazole and benzoxazole ring that are present in a number of natural products, bioactive molecules and drugs [3]. During my talk, I will present the development of new chemical entities structurally related to purine applying the scaffold hopping approach based on benzoazoles as a privileged structures. With the aim to obtain new lead compounds with improved antitumor and antibacterial activities, benzoazole and pyrrolopyrimidine derivatives were synthesized by using modern synthetic methods including click chemistry, Pd-catalyzed cross-coupling and mechanochemical reactions. [1] J. Kim et. al., J Am Chem Soc 136 (2014) 14629. [2] Y. Wan et al., Eur J Med Chem 183 (2019) 111691. [3] N. M. Meghani et al., Drug Discov Today 22 (2017) 1604.

privileged structures, benzoazoles, scaffold hopping, click chemistry

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