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In vitro anticancer effects of 1,2,4-triazole-3-carboxamides
* 1 , 2 , 1 , 2 , 1, 3, 4 , 2 , 1 , 1
1  N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia; 24 Kashirskoe Shosse, Moscow, 115478, Russia
2  MIREA - Russian Technological University, Lomonosov Institute of Fine Chemical Technologies; 78 Vernadsky Avenue, Moscow 119571, Russia
3  I.P. Pavlov Ryazan State Medical University, Ministry of Health of Russia; 9 Vysokovol’tnaya St., Ryazan, 390026, Russia
4  Peoples’ Friendship University of Russia; 6 Miklukho-Maklaya St., Moscow 117198, Russia
Academic Editor: Alfredo Berzal-Herranz (registering DOI)

Ovarian cancer (OVC) is a current health problem for women around the world. The high mortality rate from OVC makes the development of new therapeutic drugs relevant. Ribavirin (RBV, chemical name 1,2,4-triazole-3-carboxamide) is commonly used as an antiviral agent. In recent years, research has focused on repurposing RBV as an anticancer drug. However, RBV reveals a number of side effects, so synthetic derivatives of 1,2,4-triazole-3-carboxamide (TCA) are being actively developed and tested as putative anticancer drugs. The purpose of this study is to estimate the anticancer effects of RBV, TCA and its derivatives (MGs) in vitro. Cytotoxic effect of the MGs on ovarian cancer cells (OVAR3 and OVAR4) was assessed using the MTT assay. The proliferation rate of OVC cells was assessed after 72 h of treatment RBV, ТСА and MGs cell counting with trypan blue exclusion. Distribution of cell cycle phases was evaluated using flow cytometry with PI staining. RBV and MGs induced 40% cell death in OVC cells. MGs inhibited proliferation by 50-70% in OVC cells. After 72h RBV and MGs induces S-phase stunting. Furthermore, we demonstrated an increase in the number of cells in the subG1 phase (2.5%) after treatment with MG0 and MG1, as well as in G2/M-phase (10%) after treatment with MG5. According to the results obtained, 1,2,4-triazole-3-carboxamides can inhibit proliferation and induce apoptosis in vitro. These results provide the rationale for further studies of 1,2,4-triazole-3-carboxamides like anticancer drugs.

Keywords: ovarian cancer; ribavirin; 1,2,4-triazole-3-carboxamides; cell cycle