Synthesis of 7-Substituted Fluoroquinolone Derivatives Contain- ing Triazolidine Dione Moiety and In Vitro Evaluation of their Cytotoxic Effects

authors:

avatar Hadi Adibi 1 , * , avatar Leila Hosseinzadeh 1 , avatar Maryam Mahdian 2 , avatar Alireza Foroumadi 3 , avatar Mohammad Ali Zolfigol 4 , avatar Shadpour Mallakpour 5

Novel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
Student's Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran
Department of Medicinal Chemistry, Faculty of Pharmacy & Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
Faculty of Chemistry, Bu-Ali Sina University, Hamedan, Iran
Organic Polymer Chemistry Research Laboratory, Department of Chemistry, Isfahan University of Technology, Isfahan, Iran
Journal of Reports in Pharmaceutical Sciences: Vol.2, issue 1; 75-82
published online: February 25, 2013
article type: Rapid Communication
received: January 19, 2013
revised: January 29, 2013
accepted: February 18, 2013

how to cite: Adibi H, Hosseinzadeh L, Mahdian M, Foroumadi A, Zolfigol M A, et al. Synthesis of 7-Substituted Fluoroquinolone Derivatives Contain- ing Triazolidine Dione Moiety and In Vitro Evaluation of their Cytotoxic Effects. J Rep Pharm Sci. 2013;2(1):e147764. 

Abstract

A series of fluoroquinolone derivatives holding triazolidine dione moieties have been synthesized and proved to be cytotoxic agents in vitro particularly against cancer cell lines (SKNMC, MCF7, A2780-CP, SW48, A549, KB, HT-29, HepG2). The cytotoxic activity was assessed using MTT colorimetric assay. Our compounds showed less cytotoxicity than doxorubicin in all studied cell lines. The best results was obtained for the compound 3a on A549 cell line (IC50 = 34.5 μM) and the compound 3b on SW48 (IC50 = 42 μM) and A2780-CP (IC50 = 43 μM) cell lines. The compound 3b that has the phenyl urazole moiety at C-7 position, showed better anticancer effect than the compound 3a on SW48, A2780-CP and MCF7 cell lines.