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Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives

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Abstract

A series of 1-[(sub)]-6-fluoro-3- [(sub)]-1, 3, 4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro 4-quinolinones were synthesized by the reaction between ciprofloxacin and norfloxacin with an appropriate acid hydrazide in phosphorous oxychloride. All newly synthesized compounds were evaluated for their antiproliferative activities against human lung tumor cell lines (A 549). Fluoroquinolone with oxadiazole (Q 2 ) 1-cyclopropyl-6-fluoro-3- [5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl]-7-piperazino-1, 4-dihydro-4-quinolinone was found to be the most active compound in vitro with a half-maximal inhibitory concentration (IC50) of 9.0 μg/mL.

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Acknowledgement

The author (M. Shaharyar) thanks the University Grant Commission-New Delhi, India for a research award, Janab Abdul Mueed for providing the necessary facility, and Dr. Kiran Smith, National Cancer Institute-USA, for valuable suggestions.

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Authors and Affiliations

  1. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard University, Hamdard Nagar, New Delhi, 110062, India

    Mohammad Shaharyar, Mohamed Ashraf Ali & Mohammad Mustaqeem Abdullah

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  1. Mohammad Shaharyar
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  2. Mohamed Ashraf Ali
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  3. Mohammad Mustaqeem Abdullah
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Correspondence to Mohammad Shaharyar.

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Shaharyar, M., Ali, M.A. & Abdullah, M.M. Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives. Med Chem Res 16, 292–299 (2007). https://doi.org/10.1007/s00044-007-9031-x

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  • DOI: https://doi.org/10.1007/s00044-007-9031-x

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