Synthesis of novel ciprofloxacin analogues and evaluation of their anti-proliferative effect on human cancer cell lines.

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 ((1)H NMR, (13)C 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.

• Authors: Narva Suresh, Hunsur Nagendra Nagesh, Kondapalli Venkata Gowri Sekhar, Anil Kumar, Amir N Shirazi, Keykavous Parang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 23 Pg. 6292-5 (Dec 01 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 24138941 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Antineoplastic Agents
• Fluoroquinolones
• Ciprofloxacin

Topics

• Anti-Bacterial Agents (chemical synthesis, chemistry, pharmacology)
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Ciprofloxacin (analogs & derivatives, chemical synthesis, chemistry, pharmacology)
• Drug Screening Assays, Antitumor
• Fluoroquinolones (chemical synthesis, chemistry, pharmacology)
• Humans
• Molecular Structure
• Structure-Activity Relationship