Synthesis and in vitro cytotoxic activity of N-[2-(thienyl)-2-(chlorobenzyloxyimino)]ethyl enoxacin derivatives
نویسندگان
چکیده
In the present work, N-[2-(thienyl)-2-(chlorobenzyloxyimino)ethyl]enoxacin derivatives (4a-f) were synthesis by the reaction of enoxacin with 2-bromo-1-(thiophen) ethanone O-2-chlorobenzyl oxime derivatives (3a-f) in DMF in the presence of NaHCO3 at room temperature. The synthesized compounds were tested in vitro on human tumor cell lines. Preliminary screening showed 4b and 4e demonstrated significant growth inhibitory potential against all evaluated cell lines. The results of structure-activity relationship study exhibited that quinolone derivatives containing 3-chlorobenzyloxime are superior in cytotoxic potential compared to 2 and 4-chloro derivatives.
منابع مشابه
Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-activity Relationship
Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...
متن کاملNovel N-2-(Furyl)-2-(chlorobenzyloxyimino) ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-activity Relationship
Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...
متن کاملNovel N-2-(Furyl)-2-(chlorobenzyloxyimino) Ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-Activity Relationship.
Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...
متن کاملIn Vitro Cytotoxicity Evaluation of Sixteen New N-Piperazinyl Quinolone Derivatives Against A Panel Of Tumor Cell Lines
Introduction: Fluoroquinolones are potent inhibitors of bacterial topoisomerase II. They can also inhibit eukaryotic topoisomerase, and may confer antitumoral properties. Method: In this study the antitumoral activity of a new series of N-substituted piperazinylfluoroquinolones against a panel of human tumor cell lines was determined by MTT assays. Results: Among the tested compounds N-[2- (5-b...
متن کاملSynthesis of new piperazinyl quinolones and investigation of their in vitro antibacterial activities
Quinolone antibacterial agents are currently used for the treatment of various bacterial infections. The nature of functional group at the 7 position of the quinolone ring system is known to have strong influence on the spectrum and extent of in vitro antibacterial activity. Accordingly, a series of N-L2- oxo-2-(2- furyl) and N-[2- oxyimino (2- furyl) ethyl] piperazinyl quinolone derivatives...
متن کامل