Abstract:
Despite the significant progress that has been made in recent years in the treatment of cancer, tumors still represent a high risk for humanity, and therefore the development of effective cancer therapy is still a challenge for modern medicine. The choice of treatment depends on the type of cancer and its stage at the time of diagnosis. Both chemotherapy, radiotherapy and immunotherapy have a number of side effects that reduce the effectiveness of drugs and can reduce the quality of life of patients. Therefore, it is extremely important to search for new therapeutic strategies, as well as to develop drugs with a better pharmacological profile that act specifically on cancer cells and do not have a toxic effect on normal cells. The search for new lead structures involves identifying new chemical compounds that affect well-defined molecular targets. Triazine derivatives are an interesting group of compounds with potential anti-tumor activity and this scaffold has been used in oncological therapy since 1965. Since that time, a number of studies have been undertaken to modify the structure of 1,2,4-triazine derivatives, which were to provide molecules with stronger cytotoxic properties and at the same time giving fewer side effects. Thanks to this research a number of benzo- or hetero-fused 1,2,4-triazine derivatives have been found and described in the literature as new antitumor agents. Compounds in which the 1,2,4-triazine nucleus is condensed with five-membered heterocycles have received considerable attention because they are bioisosteric with purine core. Among the 1,2,4-triazine condensed with one heterocycle, compounds with pyrazolo[4,3-e][1,2,4]triazine core represent the new and most promising class with antitumor activity. Recently we have published new and very creative approach to the synthesis and functionalization of pyrazolo[4,3-e][1,2,4]triazine skeleton [1-5]. The approach is based on the intramolecular ring closure of hydrazones or substituted hydrazones of 5-acyl-1,2,4-triazines 3 involving nucleophilic substitution of hydrogen at C-6 of 1,2,4-triazine ring by the hydrazine nitrogen. The overall synthetic strategy is shown in Scheme 1.
Page(s):
93-93
DOI:
DOI not available
Published:
Journal: Abstract Book on International Conference on Life Sciences (ICLS-23) 11-12 May 22-23, Volume: 0, Issue: 0, Year: 2023