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Clonogenic long-term survival assay of HCT 116 colorectal cancer cells after treatment with the synthesized diphenyl imidazoline derivatives

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Abstract

Fourteen diphenyl imidazoline derivatives were designed, synthesized, and identified using NMR spectroscopy and high-resolution mass spectrometry. Their cytotoxicities in HCT 116 colorectal cancer cell lines were measured using a clonogenic long-term survival assay and the half-maximal cell growth inhibitory concentration (GI50) values were in the range 3.1–58.4 μM. As the anticancer effects of diphenyl imidazolines were reported to be caused by the inhibition of mouse double minute 2 homolog (MDM2), the inhibitory effects of the most potent derivative on MDM2 were assessed through Western blotting analysis. In silico docking experiments revealed the binding mode between this derivative and MDM2.

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Acknowledgments

This work was supported by the Priority Research Centers Program [NRF, 2009-0093824]. SY Shin was supported by the KU Research Professor Program of Konkuk University.

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Author notes

  1. Youngshim Lee and Dongsoo Koh contributed equally to this work,

Authors and Affiliations

  1. Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul, 05029, Republic of Korea

    Youngshim Lee, Seunghyun Ahn & Yoongho Lim

  2. Department of Applied Chemistry, Dongduk Women’s University, Seoul, 02748, Republic of Korea

    Dongsoo Koh

  3. Department of Biological Sciences, Konkuk University, Seoul, 05029, Republic of Korea

    Young Han Lee & Soon Young Shin

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  1. Youngshim Lee
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  2. Dongsoo Koh
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Correspondence to Soon Young Shin or Yoongho Lim.

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Lee, Y., Koh, D., Ahn, S. et al. Clonogenic long-term survival assay of HCT 116 colorectal cancer cells after treatment with the synthesized diphenyl imidazoline derivatives. Appl Biol Chem 61, 303–312 (2018). https://doi.org/10.1007/s13765-018-0355-7

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