Organizing co mmittee

 
 
F
O
N
H
O
N
N
HS

---

Poster presentation 
268 
CYTOTOXICITY OF 1,3,4-OXADIAZOLE-2-THIONE 
DERIVATIVES in vitro 
 
U.B. Khamidova, M.R. Umarova, E.O. Terenteva, Kh.Z. Nasriddinov, 
E.G. Yusupova, 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]  
The cytotoxic activity of several derivatives based on 5-(p-aminophenyl)-1,3,4-
oxadiazol-2-thione were studied. The cytotoxic activity of several products based on 5-
(p-aminophenyl)-1,3,4-oxadiazol-2-thione was studied. The experiment were carried out 
on cancer cell lines - cervical epithelial carcinoma HeLa, breast adenocarcinoma HBL-
100 (ATCC HTB 124), larynx adenocarcinoma Hep-2 (ATCC:CCL-23), T-
lymphoblastic leukemia CCRF-CEM (ATCC: CCL-19) and healthy cell lines - 
fibroblasts, hepatocytes, kidney cells by MTT method. The substances’ cytotoxicity was 
compared with cisplatin ("Cisplatin-Naprod", India). Testing was performed in 
triplicate, then the data was analyzed and statistically processed using Origin 8.6.
During 
the 
work, 
it 
was 
found 
that 
2-chloro-N-(4-{5-[(2-oxo-2-
phenylethyl)sulfanyl]-1,3,4-oxadiazol-2-yl}phenyl)acetamide showed high cytotoxicity 
(Fig 1.).
Figure 1. 2-chloro-N-(4-{5-[(2-oxo-2-phenylethyl)sulfanyl]-1,3,4-oxadiazol-2-
yl}phenyl)acetamide 
The IC
50
value (concentration at which 50% of the cells die) for substance was 9.8 
µM for CCRF-CEM cells, 80.1 µM for HEp-2 cells, 27.8 µM for HBL-100 cells, and 
98.8 µM for the HeLa line. 
The high cytotoxicity of this sample was also preserved on healthy cells of the body: 
the IC
50
values of this compound were higher only on liver cells - hepatocytes. 
Fibroblasts and kidney cells Vero B were highly sensitive to these derivatives - the 
values of 50% inhibition of cell growth on these lines were lower (more toxic) than on 
cancer cells. 
In conclusion, it can be said that the studied 2-chloro-N-(4-{5-[(2-oxo-2-
phenylethyl)sulfanyl]-1,3,4-oxadiazol-2-yl}phenyl)acetamide showed a higher activity 
against cancer cell lines than other derivatives. This is important in the search for anti-
cancer drugs in oncology.