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Journals / Marmara Pharmaceutical Journal / 2017 / Cilt: 21 - Sayı: 2

Toxicological Evaluation of Benzothiazole Derivatives Carrying Piperazine Ring

Mohammad CHAREHSAZ
ENİSE ECE GÜRDAL
Sinem HELVACIOĞLU
MİNE YARIM YÜKSEL
Pages
243–250
DOI
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AI Summary & Key Takeaways

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

Therefore, results demonstrate that the described molecule is promising as a new anticancer drug without mutagenicity.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Benzothiazole-piperazine derivatives prepared previously, 1h and 1j are potential anticancer agents.
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Key Findings & Data:The mutagenicity of 1h and 1j were determined by Ames test performed on Salmonella TA98 and TA100 strains.
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Conclusion & Impact:Therefore, results demonstrate that the described molecule is promising as a new anticancer drug without mutagenicity.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Özet

Benzothiazole-piperazine derivatives prepared previously, 1h and 1j are potential anticancer agents. Since the mutagenic and genotoxic properties of anticancer drugs compose an essential issue to be researched, this study is focused on the analysis of the mutagenicity and genotoxicity of these molecules. The mutagenicity of 1h and 1j were determined by Ames test performed on Salmonella TA98 and TA100 strains. Sample 1j was mutagenic on TA98 bacterial strain. However, compound 1h was not mutagenic in bacterial strains TA98 and TA100 with and without S9 activation. The genotoxicity of 1h was evaluated by the chromosomal aberration assay on human lymphocytes. Compound 1h was also not genotoxic in human lymphocytes in vitro. All results revealed that, 1h was not mutagenic in the two Salmonella strains tested and was not genotoxic in chromosomal aberration assay. Therefore, results demonstrate that the described molecule is promising as a new anticancer drug without mutagenicity. Also, after performing Ames test with other recommended bacterial strains and in vivo experiments can be used safely for the development of new structures exhibiting anticancer activities.

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Cite This Article

CHAREHSAZ, M., GÜRDAL, E. E., HELVACIOĞLU, S., YÜKSEL, M. Y. (2017). Toxicological Evaluation of Benzothiazole Derivatives Carrying Piperazine Ring. Marmara Pharmaceutical Journal, Cilt: 21 - Sayı: 2, 243–250. https://ajindex.com/articles/283751

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References (12)

  1. Klaunig JE, Kamendulis LM. Chemical carcinogenesis. In: Casarett & Doull’s Toxicology the Basic Sciences of Poisons. Editor: Klaassen CD. McGraw-Hill Companies, Inc. Philadelphia. 2008, pp.329-379.
  2. Lucy H, Golsteyn S, Golsteyn RM. Genotoxic anti-cancer agents and their relationship to DNA damage, mitosis, and checkpoint adaptation in proliferating cancer cells. Int J Mol Sci 2014; 15: 3403-31.
  3. Helleday T, Petermann E, Lundin C, Hodgson B, Sharma RA. DNA repair pathways as targets for cancer therapy. Nat Rev Cancer 2008; 8: 193–204.
  4. Charehsaz M, Onen-Bayram FE, Sipahi H, Buran K, Giri AK, Aydin A. Evaluation of the mutagenic and genotoxic effects of the ALC67 thiazolidine compound in Salmonella strains and human lymphocytes in vitro. Hum Exp Toxicol 2016; 35: 1108–15.
  5. Yamazaki K, Kaneko Y, Suwa K, Ebara S, Nakazawa K, Yasuno K. Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure. Bioorg Med Chem 2005; 13: 2509-22.
  6. Brantley E, Antony S, Kohlhagen G, Meng L, Agama K, Stinson SF, Sausville EA, Pommier Y. Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells. Cancer Chemother Pharmacol 2006; 58: 62-72.
  7. Lion CJ, Matthews CS, Wells G, Bradshaw TD, Stevens MF, Westwell AD. Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones Charehsaz et al. (‘quinols’). Bioorg Med Chem Lett 2006; 16: 5005-8.
  8. Huang ST, Hsei IJ, Chen C. Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles. Bioorg Med Chem 2006; 14: 6106-19.
  9. Yoshida M, Hayakawa I, Hayashi N, Agatsuma T, Oda Y, Tanzawa F, Iwasaki S, Koyama K, Furukawa H, Kurakata S, Sugano Y. Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents. Bioorg Med Chem Lett 2005; 15: 3328-32.
  10. Das J, Moquin RV, Lin J, Liu C, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, Barrish JC, Wityak J. Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors. Bioorg Med Chem Lett 2003; 13: 2587-90.
  11. Noolvi MN, Patel HM, Kaur M. Benzothiazoles: search for anticancer agents. Eur J Med Chem 2012; 54: 447-62.
  12. Gurdal EE, Buclulgan E, Durmaz I, Cetin-Atalay R, Yarim M. Synthesis and anticancer activity evaluation of some benzothiazole-piperazine derivatives. Anticancer Agents Med Chem 2015; 15: 382-9.