Investigation of cytotoxic effects of some novel synthesized iminothiazolidinone derivatives on HeLa cell line (CCL2)
Öz
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.
Anahtar Kelimeler
Iminothiazolidinone HeLa cells viability mitotic index labelling index
Kaynakça
- 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.
Öz
Kaynakça
- 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.
Ayrıntılar
| Bölüm | Araştırma Makaleleri |
|---|---|
| Yazarlar | |
| Yayımlanma Tarihi | 3 Mayıs 2017 |
| Gönderilme Tarihi | 3 Mayıs 2017 |
| Yayımlandığı Sayı | Yıl 2016 Cilt: 75 Sayı: 1 |
