Journals / IUFS Journal of Biology / 2016 / Cilt: 75 - Sayı: 1

Bazı yeni sentezlenmiş iminotiazolidinon türevlerinin HeLa hücre hattı üzerindeki sitotoksik etkilerinin araştırılması

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

Pages
39–49
Publication Date
2022-10-18
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

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.

📌 3 Key Takeaways

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Objective & Hypothesis:In medicinal chemistry, the thiazolidinones are a practical framework which can be leaned as a pharmacophore in a large diversity of biologically active compounds.
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Key Findings & Data: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.
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Conclusion & Impact: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.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

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, antiHIV 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

Özet

Tıbbi kimyada, tiazolidinonlar, büyük bir çeşitlilik barındıran biyolojik olarak aktif bileşikler içinde farmokofor olarak kullanılabilecek kapasiteye sahiptir. Ayrıca, birçok terapötik ajanlarda antibakteriyel, anti-konvülsan, anti-tümöral, antiviral, anti-diyabetik, anti-inflamatuar ve anti-HIV bileşiklerinin tabanını oluştururlar. Bu çalışmada, bazı yeni sentezlenmiş iminotiazolidinon türevlerinin (A-E Bileşikleri) insan servikal karsinomu kaynaklı HeLa (3) hücre hattı (CCL2) üzerine sitotoksik etkileri araştırılmıştır. Buna göre iminotiazolidinon türevlerinin uygulanması üzerine yayılma hızı, mitotik ve işaretlenme indeksinin kinetik parametreleri belirlenmiştir. Optimum konsantrasyonların bulunması için 1x10-6, 5x10-6, 10x10-6M konsantrasyonlarında tiazolidinon türevleri 72 saat süreyle uygulanmış ve sonuç, üreme hızı analizi ile açıklanmıştır. 0-72 saat boyunca benzersiz şekilde sentezlenmiş iminotiazolidinon türevlerinin optimum konsantrasyonları ile muamele edilen hücrelerin mitotik ve işaret indeks parametreleri hesaplanmıştır. Sonuç olarak, test edilen bileşiklerin HeLa hücre kültürlerinin çoğalmasında, kayda değer bir düşüşe neden olduğu ve 10x10-6 M konsantrasyondaki iminotiazolidinon türevlerinin çoğalma hızının düşüşüne ilişkin en etkili konsantrasyon olduğu bulunmuştur. Bu türevlerden elde edilecek ilaçların gelecekte serviks karsinoması tedavisinde umut verici bir model sunması ümit edilmektedir

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Cite This Article

ÇETİN, İ., GERÇEK, Y. C., TOPÇUL, M. R., ÇALIŞKAN, M., ÖZ, G. C., TUĞCU, T. F., MORGİL, H., ÜNLÜ, Y. S. (2022). Bazı yeni sentezlenmiş iminotiazolidinon türevlerinin HeLa hücre hattı üzerindeki sitotoksik etkilerinin araştırılması. IUFS Journal of Biology, Cilt: 75 - Sayı: 1, 39–49. https://ajindex.com/articles/543989

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References (10)

  1. Amit Verma A. and Saraf K.S. (2008) 4-Thiazolidinone - A biologically active scaffold. Eur J Med Chem., 43: 897-905.
  2. 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 Chem., 17(6): 2576-84.
  3. Chavan A.A. and Pai N.R. (2007) Synthesis and antimicrobial screening of 5-arylidene- 2-imino-4-thiazolidinones. Arkivoc, 16: 148-55.
  4. Hamama W.S., Ismail M.A., Shaaban S. and Zoorob H.H. (2008) Progress in the Chemistry of 4-Thiazolidinones. J Heterocyclic Chem., 45(4): 939-56.
  5. Hamama W.S., Zoorob H.H., Gouda M.A. and Afsah E.M (2011) Synthesis and antimicrobial and antioxidant activities of simple saccharin derivatives with N-basic side chains. Pharm Chem J., 45(2): 118-24.
  6. Havrylyuk D., Zimenkovsky B., Vasylenko O., Zaprutko L., Gzella A. and Lesyk R (2009) Synthesis of novel thiazolonebased compounds containing pyrazoline moiety and evaluation of their anticancer activity. Eur J Med Chem., 44(4): 1396- 1404. Havrylyuk D., Mosula L., Zimenkovsky B., Vasylenko O., Gzella A. and Lesyk R. (2010) Synthesis and anticancer activity evaluation of 4-thiazolidinones containing benzothiazole moiety. Eur J Med Chem., 45(11): 5012-21.
  7. Jain K.A., Vaidya A., Ravichandran V., Kashaw.KS., Agrawal K.R. (2012) Recent developments and biological activities of thiazolidinone derivatives: A review. Bioorgan Med Chem., 20 (11): 3378-95. Kaminskyy D., den Hartog G. J., Wojtyra M., Lelyukh M., Gzella A., Bast, A. and Lesyk R (2016) Antifibrotic and anticancer action of 5-ene amino/ iminothiazolidinones. European Journal of Medicinal Chemistry, 112: 180-95.
  8. Kasmi-Mir S., Djafri A., Paquin L., Hamelin J. and Rahmouni M. (2006) One-pot synthesis of 5-arylidene-2-imino- 4-thiazolidinones under microwave irradiation. Molecules, 11: 597-602.
  9. Kumar K.S.S., Hanumappa A., Hegde M., Narasimhamurthy K.H., Raghavan S.C. and Rangappa K.S (2014) Synthesis and antiproliferative effect of novel 4- thiazolidinone-, pyridine- and piperazinebased conjugates on human leukemic cells. Eur. J. Med. Chem. 81: 341-49.
  10. Küçükgüzel İ., Tatar E., Küçükgüzel G., Rollas S. and Clercq D.E. (2008) Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4- alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole- 3-thiones and