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Tridentate bipyrazole compounds with a side-arm as a new class of antitumor agents

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Abstract

Eight tridentate bipyrazole derivatives with different side arms have been prepared in one step and with good yields. The products were screened for their cytotoxic activity against three tumor cell lines—human breast cancer cell line MDA-MB231, human prostate cancer cell line PC3, and human colorectal cell line LoVo, by use of colorimetric MTT assay. Structure–activity relationships reflected the effect of substituted drugs. Among this series, two compounds had remarkable in-vitro antiproliferative activity against the LoVo cell line with IC50 values ranging from 2.6 to 2.7 μg ml−1. All the compounds had suitable drug-like characteristics according to Lipinski’s rule.

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Acknowledgments

This work was supported by the CUD (Commission Universitaire pour le Développement, Belgium) within the framework of the P3 program.

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Authors and Affiliations

  1. LCOMPN-URAC 25, Facultés des Sciences, Université Mohamed I, Oujda, Morocco

    Fouad Malek

  2. Angiogenesis and Cancer Research Lab, Pole of Pharmacology and Therapeutics—FATH5349, Institute of Experimental and Clinical Research, UCL, Brussels, Belgium

    Nihed Draoui & Olivier Feron

  3. LCAE, Chemistry Department, Sciences Faculty, Mohamed the First University, Oujda, Morocco

    Smaail Radi

Authors
  1. Fouad Malek
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  2. Nihed Draoui
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  3. Olivier Feron
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  4. Smaail Radi
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Correspondence to Smaail Radi.

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Malek, F., Draoui, N., Feron, O. et al. Tridentate bipyrazole compounds with a side-arm as a new class of antitumor agents. Res Chem Intermed 40, 681–687 (2014). https://doi.org/10.1007/s11164-012-0993-z

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  • DOI: https://doi.org/10.1007/s11164-012-0993-z

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