Investigation of cytotoxic effects of some novel synthesized iminothiazolidinone derivatives on HeLa cell line (CCL2)

In medicinal chemistry, the thiazolidinones are a practical framework which can be leaned as a pharmacophore in a large diversity of biologically active compounds. Furthermore, they build up the base of antibacterials, anti-convulsant, anti-tumorals, antivirals, anti-diabetic, anti-inflammatory, anti- HIV compounds in many other therapeutic agents. In this study, the cytotoxic effects of some novel synthesized iminothiazolidinone derivatives (Compound A-E) on HeLa (3) cell line (CCL2) which arising from human cervical carcinoma were studied. Accordingly, kinetics parameters of proliferation rate, mitotic and the labeling index were determined upon the application of the iminothiazolidinone derivatives. 1 x 10-6, 5 x 10-6, 10 x 10-6 M concentrations of the derivatives were implemented for 72 hours to find out the optimum concentrations, and the result was explicated by reproduction rate analysis. Parameters of the mitotic and labeling index of the cells which were treated with the optimum concentrations of the uniquely synthesized iminothiazolidinone derivatives for 0-72 hours were calculated. The results indicated that the tested compounds caused a remarkable decrease in the propagation of HeLa cell cultures and the 10 x 10-6 M concentration was found to be the most effective concentration of the iminothiazolidinone derivatives regarding reducing the reproduction rate. Drugs can be obtained from these derivatives will offer a promising treatment modality in cervix carcinoma in the future. 

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  • Amit Verma A. and Saraf K.S. (2008) 4-Thiazolidinone – A biologically active scaffold. Eur J Med Chem., 43: 897–905. Chandrappa S, Kavitha C.V, Shahabuddin M.S, Vinaya K, Kumar C.S, Ranganatha S.R, Raghavan S. and Rangappa K.S. (2009) Synthesis of 2-(5-((5-(4-chlorophenyl) furan-2-yl)methylene)-4-oxo-2- thioxothiazolidin-3-yl) acetic acid derivatives and evaluation of their cytotoxicity and induction of apoptosis in human leukemia cells. Bioorgan Med Tuğcu et al. / IUFS Journal of Biology 2016, 75(1): 39-49 49 Modeling of Antitumor Activity. Current Topics Med Chem., 12 (24): 2763-84. Ottana R., Maccari R., Barreca M.L., Bruno G., Rotondo A., Rossi A., Chiricosta G., Di Paola R., Sautebin L., Cuzzocrea S.E. and Vigorita M.G. (2005) 5-Arylidene- 2-imino-4-thiazolidinones: design and synthesis of novel anti-in ammatory agents. Bioorgan Med Chem., 13:4243– 52. Panchuk R.R., Chumak V.V., Fil R.M., Havrylyuk Y.D., Zimenkovsky B.S., Lesyk R.B. and Stoika R.S. (2012) Study of molecular mechanisms of proapoptotic action of novel heterocyclic 4-thiazolidone derivatives. Biopoly and Cell, 28(2): 121-28. Rahman V.P., Mukhtar S., Ansari H.W. and Lemiere G. (2005) Synthesis, stereochemistry and biological activity of some novel long alkyl chain substituted thiazolidin-4-ones and thiazan-4-one from 10-undecenoic acid hydrazide. Eur J Med Chem., 40(2): 173–84 Tuğcu, T. (2009) Multikomponent yöntemiyle yeni hetaril sustitue iminotiyazolidinon bileşiklerinin sentezi / Synthesis of new hetaryl substituted iminothiazolidinone compounds via the multicomponent method. Yüksek Lisans Tezi, Yıldız Teknik Üniversitesi, Fen Bilimleri Enstitüsü. Verma A. and Saraf S.K. (2008) 4-thiazolidinone--a biologically active scaffold. Eur J Med Chem.,43: 897-905. Wilson C., Claudia G., Vellasco J.R. and Walcimar T. (2008) Chemistry and Biological Activities of 1,3-Thiazolidin- 4-ones. Mini-Rev Organ Chem., 5(4): 336-44.
European Journal of Biology-Cover
  • ISSN: 2602-2575
  • Yayın Aralığı: Yılda 2 Sayı
  • Başlangıç: 1940
  • Yayıncı: İstanbul Üniversitesi Yayınevi