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A novel radiolabeled indole derivative as solid tumor imaging agent: in silico and preclinical pharmacological study

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Abstract

Biologically active indole derivative was synthesized and screened for its cytotoxicity against breast cancer cell line (MCF-7) with the IC50 equals 17.5 µg/mL. Docking study showed its high binding affinity to the COX-2 enzyme. It’s radiolabeling with 99mTc and showed high radiochemical yield (92.10 ± 0.57%) and in vitro stability in serum up to 10 h. Biodistribution studies of a novel 99mTc-NSIC complex in tumor-bearing mice showed high T/NT ratio (6.17 ± 0.08 at 30 min. post-injection), suggesting this complex could be used as a solid tumor imaging agent.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    H. A. Shamsel-Din & A. B. Ibrahim

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  1. H. A. Shamsel-Din
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  2. A. B. Ibrahim
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Correspondence to H. A. Shamsel-Din.

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Shamsel-Din, H.A., Ibrahim, A.B. A novel radiolabeled indole derivative as solid tumor imaging agent: in silico and preclinical pharmacological study. J Radioanal Nucl Chem 314, 2263–2269 (2017). https://doi.org/10.1007/s10967-017-5551-0

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  • DOI: https://doi.org/10.1007/s10967-017-5551-0

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