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RESEARCH ARTICLE
Contents Vol 66(6)

Synthesis and Cytotoxicity Evaluation of Some Novel 1-(3-Chlorophenyl)piperazin-2-one Derivatives Bearing Imidazole Bioisosteres

Saeed Ghasemi A , Simin Sharifi C D , Soodabeh Davaran A C D , Hosein Danafar A , Davoud Asgari A C and Javid Shahbazi Mojarrad A B E
+ Author Affiliations
- Author Affiliations

A Department of Medicinal Chemistry, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran.

B Tuberculosis and Lung Disease Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran.

C Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz 51664, Iran.

D Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran.

E Corresponding author. Email: jvshahbazi@yahoo.com

Australian Journal of Chemistry 66(6) 655-660 https://doi.org/10.1071/CH13031
Submitted: 19 January 2013  Accepted: 22 February 2013   Published: 25 March 2013

Abstract

A series of substituted 3-chlorophenylpiperazinone derivatives were synthesised using L-778123 (an imidazole-containing FTase inhibitor) as a model by bioisosteric replacement of the imidazole ring. The final compounds were evaluated against two human cancer cell lines including A549 (lung cancer) and HT-29 (colon cancer) by MTT assay. The results showed that substitution of imidazole ring with 1-amidinourea, semicarbazide, and thiobiuret led to improvement of cytotoxic activity against both cell lines.


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