European Journal of Chemistry 2012, 3(3), 356-358. doi:10.5155/eurjchem.3.3.356-358.621

Anticancer activity studies of some cyclic benzimidazole derivatives

Ali El-Shekeil (1,*) , Abeer Omer Obeid (2) , Sama Al-Aghbari (3)

(1) Chemistry Department, Faculty of Science, Sana’a University, 2463, Sana’a, Yemen
(2) Chemistry Department, Faculty of Science, Sana’a University, 2463, Sana’a, Yemen
(3) Chemistry Department, Faculty of Science, Sana’a University, 2463, Sana’a, Yemen
(*) Corresponding Author

Received: 23 Apr 2012, Accepted: 17 Jun 2012, Published: 30 Sep 2012


New benzimidazole derivatives, namely, (N-(4-methoxyphenyl)methylene]-1H-benzimidazol-2-amine (2a), (N-(3,4-dimethoxyphenyl)methylene]-1H-benzimidazol-2-amine (2b), and (N-(3,4,5-trimethoxyphenyl)methylene]-1H-benzimidazol-2-amine (2c) were synthesized by reaction of a Schiff base with malononitrile in absolute ethanol. Structures of compounds have been confirmed by IR, 1H NMR and elemental analysis. Compounds 2a-c were screened for their in vitro anticancer potential using HeLa and PC3 cells. All compounds showed limited cytotoxicity except compound 2a that showed a moderate cytotoxic effect towards HeLa cells.



PC3 cells; Hela cells; Cytotoxicity; Anti-cancer activity; Benzimidazole derivatives; 4-Amino-2-(3,4,5-trimethoxyphenyl)benzo[4,5]imidazo[1,2-a]pyrimidine-3-carbonitrile

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DOI: 10.5155/eurjchem.3.3.356-358.621

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[1]. Ramla, M. M.; Omer, M. A.; El-Khamry, A. M. M.; El-Diwani, H. I. Bioorg. Med. Chem. 2006, 14, 7324-7332.

[2]. Yang, Y. H.; Cheng, M. S.; Wang, Q. H.; Nie, H.; Liao, N.; Wang, J.; Chen, H.; Design. Eur. J. Med. Chem. 2009, 44, 1808-1812.

[3]. Penning, T. D.; Zhu, G. D.; Gandhi, V. B.; Gong Thomas, S. J.; Lubisch, W.; Gradel, R.; Wernet, W.; Park, C. H.; Fry, E. H.; Liu X.; Shi, Y.; Klinghofer, V.; Johnson, E. F.; Donawho, C. K.; Frost, D. J.; Diaz, V. B.; Bouska, J. J.; Olson, A. M.; Marsh, K. C. Bioorg. Med. Chem. 2008, 16, 6965-6975.

[4]. Garuti, L.; Roberti, M.; Pizzirani, D.; Pession A.; Leoncini, E.; Cenci, V.; Hrelia, S. Il Farmaco 2004, 59, 663-668.

[5]. Spasov, A. R.; Iezhitsa, I. N.; Bugaeva, L. I.; Anisimova, V. A. Khim. Farm. Zh. 1999, 33, 6-12.

[6]. Parshanth, A.; David, W. W. J. Am. Chem. Soc. 2009, 131, 7618-7624.
PMid:19445463 PMCid:2698132

[7]. Klimesova, V.; Koci, J.; Pour, M.; Stachel, J.; Waisser, K.; Kaustova, J. Eur. J. Med. Chem. 2002, 37, 409-420.

[8]. Sondhi, S. M.; Singhal, N.; Johar, M.; Reddy, B. S.; Lown, J. W. Curr. Med. Chem. 2002, 9, 1045-1074.

[9]. Demirayak, S.; Mohsen, U. A.; Karaburun, A. C. Eur. J. Med. Chem. 2002, 37, 225-260.

[10]. Huang, S. T.; Hsei, I. J.; Chen, C. Bioorg. Med. Chem. 2006, 14, 6106-6119.

[11]. Boiani, M.; Gonzalez, M. Mini-Rev. Med. Chem. 2005, 5, 409-424.

[12]. Hori, A.; Imaeda, Y.; Kubo, K.; Kusaka, M. Cancer lett. 2002, 183, 53-62.

[13]. Nawrocka, W; Sztuba, B.; Kowalska, M. W.; Liszkiewicz, H.; Wietrzyk, J.; Nasulewicz, A.; Pelczynska, M.; Opolski, A. Il Farmaco 2004, 59(2), 83-91.

[14]. Mosmann, T. J. Immunol. Methods 1983, 65(1-2), 55-63.

How to cite

El-Shekeil, A.; Obeid, A.; Al-Aghbari, S. Eur. J. Chem. 2012, 3(3), 356-358. doi:10.5155/eurjchem.3.3.356-358.621
El-Shekeil, A.; Obeid, A.; Al-Aghbari, S. Anticancer activity studies of some cyclic benzimidazole derivatives. Eur. J. Chem. 2012, 3(3), 356-358. doi:10.5155/eurjchem.3.3.356-358.621
El-Shekeil, A., Obeid, A., & Al-Aghbari, S. (2012). Anticancer activity studies of some cyclic benzimidazole derivatives. European Journal of Chemistry, 3(3), 356-358. doi:10.5155/eurjchem.3.3.356-358.621
El-Shekeil, Ali, Abeer Omer Obeid, & Sama Al-Aghbari. "Anticancer activity studies of some cyclic benzimidazole derivatives." European Journal of Chemistry [Online], 3.3 (2012): 356-358. Web. 17 Sep. 2019
El-Shekeil, Ali, Obeid, Abeer, AND Al-Aghbari, Sama. "Anticancer activity studies of some cyclic benzimidazole derivatives" European Journal of Chemistry [Online], Volume 3 Number 3 (30 September 2012)

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