Organizing co mmittee

2 
in the crystal. 
 
 

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Poster presentation 
227 
SYNTHESIS OF N-(R-PHENYL)-(4,5-DIPHENYL-1,2,4-TRIAZOL-3-
YLTHIO)ACETOHYDRAZONES AND THEIR CYTOTOXIC 
ACTIVITY 
A.A. Ziyaev
1
, E.O. Terenteva
1
, B.N. Babaev
2
, T.T. Toshmurodov
1
 
1) S.Yu. Yunusov Institute of the Chemistry of Plant Substances, Academy of Sciences of 
the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, Uzbekistan 
e-mail: [e-mail] 
2) National University of Uzbekistan 
Recently, derivatives of 1,2,4-triazoles and their thio-analogues - 1,2,4-triazole-3-
thiones have received much attention due to their chemical and different biological 
activity. Drugs containing a 1,2,4-triazole cycle such as fluconazole, itraconazole, 
voriconazole, triazolam, alprazolam, etizolam, etc. are widely used in medical practice 
[2]. In order to search for new biologically active derivatives of 1,2,4-triazole, we have 
synthesized N-(R-phenyl)-(4,5-diphenyl-1,2,4-triazol-3-ylthio)acetohydrazones (3-6) 
and their cytotoxic activity was studied: 
By reacting equimolar amounts of ethyl ester[(4,5-diphenyl)-1,2,4-triazol-3-
ylthio]acetic acid (1) with hydrazine hydrate in ethanol, hydrazide[(4,5-diphenyl)-1,2,4-
triazol-3-ylthio]acetic acid (2) was synthesized in high yield (89%). Further, by 
condensation of 2 with aromatic aldehydes at a molar ratio of reagents of 1:1.2 with 
boiling in an alcoholic solution, the corresponding acetohydrazones (3–6) were obtained 
in 79–87% yields. The cytotoxic properties of the compounds were determined by the in 
vitro MTT method [2] on cell cultures of cervical epithelial carcinoma HeLa, breast 
adenocarcinoma HBL-100, laryngeal adenocarcinoma HEp-2, and T-lymphoblastic 
leukemia CCRF-CEM; Cytostatic Cisplatin-Naprod (India) was used as a positive 
control. According to the test results, the inhibition of cell growth of the studied 
compounds in relation to the HEP-2 and HBL-100 lines varied within 47-59%, while 
their activity was minimal on other cells. 
Referenses 
1. P. Kaur et al. 1,2,4-Triazole: a revive of pharmacological activities Int. Res. J. 
Pharm. 2017, 8(7), p. 10-29. 
2. Niks M., Otto M. Towards an optimized MTT assay// Journal of Immunological 
Methods, 1990, 130, p.149-151. 

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Poster presentation 
228