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Novel brominated quinoline and pyrimidoquinoline derivatives as potential cytotoxic agents with synergistic effects of γ-radiation

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Abstract

New quinoline derivatives 6, 7 and 19, pyrimidoquinoline derivatives 8–16 and triazolopyrimidoquinoline derivatives 17 and 18 bearing a bromo-substituent were synthesized starting from 3-(4-Bromophenylamino)-5,5-dimethylcyclohex-2-enone 3. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 9, 11, 17 and 18 showed IC50 values (36.4, 39.7, 39.02 and 36.4 μM, respectively) comparable to that of the reference drug doxorubicin (IC50 = 32.02 μM). On the other hand, compound 6, 14 and 19 exhibited better activity than doxorubicin with IC50 values of 8.5, 23.5 and 23.7 μM. Additionally, the most potent compounds 6, 14 and 19 were evaluated for their ability to enhance the cell killing effect of γ-radiation.

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Authors and Affiliations

  1. Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia

    Mostafa M. Ghorab

  2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

    Fatma A. Ragab & Yassin M. Nissan

  3. Department of Drug Radiation Research, National Centre for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt

    Helmi I. Heiba & Walid M. Ghorab

Authors
  1. Mostafa M. Ghorab
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  2. Fatma A. Ragab
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  3. Helmi I. Heiba
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  4. Yassin M. Nissan
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  5. Walid M. Ghorab
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Correspondence to Mostafa M. Ghorab.

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Ghorab, M.M., Ragab, F.A., Heiba, H.I. et al. Novel brominated quinoline and pyrimidoquinoline derivatives as potential cytotoxic agents with synergistic effects of γ-radiation. Arch. Pharm. Res. 35, 1335–1346 (2012). https://doi.org/10.1007/s12272-012-0803-6

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  • DOI: https://doi.org/10.1007/s12272-012-0803-6

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