Organizing co mmittee

STUDY OF CYTOTOXIC ACTIVITY OF OXADIAZOLE 
DERIVATIVES 
 
M.R. Umarova, U.B. Khamidova, E.O. Terenteva, G.A. Piyakina, 
G.Ya. Khashimova, D.S. Ismailova, B.J. Elmuradov, Sh.S. Azimova 
 
S.Yu. Yunusov Institute of the Chemistry of Plant Substances Academy of 
sciences of the Republic of Uzbekistan st. Mirzo-Ulugbek, 77, 100170 Tashkent
e-mail: [e-mail] 
 
In this work, cytotoxic activity of several products based on 5-(p-aminophenyl)-
1,3,4-oxadiazol-2-thione was studied were studied. These samples were tested for 
cytotoxicity on 4 cancer cell lines (epithelial carcinoma of the cervix HeLa, breast 
adenocarcinoma HBL-100 (ATCC HTB 124) and adenocarcinoma of the larynx HEp-2 
(ATCC:CCL-23), T-lymphoblastic leukemia CCRF-CEM (ATCC:CCL-19)) by the 
MTT method. 
Substances were dissolved in DMSO (0.8% by volume) and introduced into cells at a 
concentration of 1 μM, 10 μM, 30 μM, 50 μM, 70 μM, 100 μM. Cell viability was 
determined by the ratio of living cells exposed to the test substance to the number of 
living cells in the control. The well-known anticancer drug cisplatin was used as the 
reference drug. 
Figure 1. 4-fluoro-N-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)benzamide 
Among 
the 
tested 
samples 
4-fluoro-N-(4-(5-mercapto-1,3,4-oxadiazol-2-
yl)phenyl)benzamide mono exhibited pronounced cytotoxicity (Fig 1): the IC
50
value 
for breast adenocarcinoma HBL-100 cells was 30.9 μM, for cervical carcinoma HeLa 
cells, 54.6 μM, and for T-lymphoblastic leukemia CCRF-CEM, 31.4 μM. The laryngeal 
adenocarcinoma line Hep-2 was not very sensitive to the action of this derivative - the 
IC
50
value was only 79.7 μM. The cytotoxic effect of this compound was preserved 
even against healthy cell cultures: the IC
50
values of this compound showed a high 
value only in liver cells - hepatocytes. Fibroblasts and Vero B kidney cells were also 
very sensitive to this derivative - the values of 50% inhibition of cell growth in these 
lines were lower (more toxic) than in cancer cells. 
The experiments reveal that the studied substances can be tested on other types of 
cancer cells. This is important in the search for anti-cancer agents.