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Synthesis of novel ciprofloxacin analogues and evaluation of their anti-proliferative effect on human cancer cell lines
Authors:Narva Suresh  Hunsur Nagendra Nagesh  Kondapalli Venkata Gowri Chandra Sekhar  Anil Kumar  Amir N Shirazi  Keykavous Parang
Institution:1. Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India;2. Department of Chemistry, Birla Institute of Technology & Science, Pilani 333 031, Rajasthan, India;3. Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA
Abstract:A series of twenty two novel 1-cyclopropyl-6-fluoro-4-oxo-7-(4-substituted piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid analogues have been synthesized, characterized (1H NMR, 13C NMR and LCMS) and evaluated for their inhibitory activity on the proliferation of human caucasian acute lymphoblastic leukemia cells (CCRF-CEM), breast adenocarcinoma cells (MDA-MB-468) and human colon carcinoma cells (HCT-116). Among all the synthesized ciprofloxacin analogues 3t at 50 μM showed comparable potency to doxorubicin (10 μM) in all three cell lines and 3j inhibited proliferation of MDA-MB-468 up to 35% selectively over other two cell lines.
Keywords:Ciprofloxacin  Fluoroquinolones  Anti-cancer  Anti-proliferative  Substituted piperazines
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