Biopolym. Cell. 2023; 39(1):33-41.
http://dx.doi.org/10.7124/bc.000A86
Bioorganic Chemistry
Study of the anticancer activity of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide toward human tumor cells in vitro
1Finiuk N. S., 2Drapak I. V., 2Zimenkovsky B. S., 1Stoika R. S.
  1. Institute of Cell Biology, NAS of Ukraine
    14/16, Drahomanov Str., Lviv, Ukraine, 79005
  2. Danylo Halytsky Lviv National Medical University
    69, Pekarska Str., Lviv, Ukraine, 79010

Abstract

Aim. In vitro study and characterization of anticancer activity of new heterocyclic derivative – N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide. Methods. The cell culture; MTT assay. Results. We synthesized N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide, which possessed diuretic, cardioprotective, and anti-inflammatory effects. Here, we investigated its cytotoxicity effect towards the tumor cell lines of various tissue origins: liver (HepG2), breast (MCF-7), lung (A549), cervical (KB3-1), and leukemia (HL-60) cells, as well as towards the non-tumor cells (HEK293 and NIH3T3). The IC50 values of the synthesized compound for tumor cells were in the range of 9.4-97.6 μg/mL. We found that the human hepatocellular carcinoma HepG2 cells were the most sensitive to the action of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide with the IC50 value of 9.4 μg/mL. The studied derivative slightly inhibited the growth of the pseudo-normal HEK293 and NIH3T3 cells. Conclusions. The anti-proliferative activity of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide dropped in the order: hepatocarcinoma > leukemia > breast carcinoma cells. Thus, we revealed in the molecule of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide a combination of the diuretic, cardioprotective, anti-inflammatory and anticancer activities, which is of great significance for this agent as a potent anticancer medicine.
Keywords: N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide, cytotoxicity in vitro, anticancer activity
Full text: (PDF, in English)

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