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Synthesis and biological evaluation of novel resveratrol-oxadiazole hybrid heterocycles as potential antiproliferative agents

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Abstract

A novel class of resveratrol-oxadiazole hybrid compounds was synthesized to screen for their in vitro antiproliferative activity against three human cancer cell lines. All the compounds showed superior antiproliferative activity than the reference compound resveratrol. The most promising active compounds in this series were 1g, 2g, 1c, 2c, 2i and 1a (GI50 < 0.1 µM), endowed with excellent antiproliferative activity. Thus, we believe that resveratrol-oxadiazole hybrid compounds may possibly be used as a good leads for the development of new antiproliferative agents. Structures of newly synthesized compounds were confirmed by NMR and IR spectral data.

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Acknowledgments

The authors are thankful to the Director, Indian Institute of Chemical Technology, Hyderabad, for the encouragement, RP thankful to CSIR, New Delhi, India for the award of research fellowships. We thank CSIR for financial support under the 12th Five Year plan projects ‘‘Affordable Cancer Therapeutics (ACT)’’ (CSC 0301) and ‘‘Small Molecules in Lead Exploration (SMiLE)’’ (CSC0111).

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Authors and Affiliations

  1. Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, Indian Institute of Chemical Technology, Uppal Road, Hyderabad, 500007, India

    M. S. R. Murty & Raju Penthala

  2. Centre for Chemical Biology, Indian Institute of Chemical Technology, Uppal Road, Hyderabad, 500007, India

    Sowjanya Polepalli & N. Jain

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  1. M. S. R. Murty
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  2. Raju Penthala
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  3. Sowjanya Polepalli
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  4. N. Jain
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Correspondence to M. S. R. Murty.

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Murty, M.S.R., Penthala, R., Polepalli, S. et al. Synthesis and biological evaluation of novel resveratrol-oxadiazole hybrid heterocycles as potential antiproliferative agents. Med Chem Res 25, 627–643 (2016). https://doi.org/10.1007/s00044-016-1514-1

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