Novel Structural Insight into Inhibitors of Heme Oxygenase-1 (HO-1) by New Imidazole-Based Compounds: Biochemical and In Vitro Anticancer Activity Evaluation

@article{Greish2018NovelSI,
  title={Novel Structural Insight into Inhibitors of Heme Oxygenase-1 (HO-1) by New Imidazole-Based Compounds: Biochemical and In Vitro Anticancer Activity Evaluation},
  author={K. Greish and L. Salerno and Reem Al Zahrani and E. Amata and M. Modica and G. Romeo and A. Marrazzo and O. Prezzavento and V. Sorrenti and A. Rescifina and Giuseppe Floresta and Sebastiano Intagliata and V. Pittal{\`a}},
  journal={Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry},
  year={2018},
  volume={23}
}
  • K. Greish, L. Salerno, +10 authors V. Pittalà
  • Published 2018
  • Chemistry, Medicine
  • Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
In this paper, the design, synthesis, and molecular modeling of a new azole-based HO-1 inhibitors was reported, using compound 1 as a lead compound, in which an imidazole moiety is linked to a hydrophobic group by means of an ethanolic spacer. The tested compounds showed a good inhibitor activity and possessed IC50 values in the micromolar range. These results were obtained by targeting the hydrophobic western region. Molecular modeling studies confirmed a consolidated binding mode in which the… Expand
28 Citations
New Arylethanolimidazole Derivatives as HO-1 Inhibitors with Cytotoxicity against MCF-7 Breast Cancer Cells
  • 4
  • PDF
Effective Virtual Screening Strategy toward heme-containing proteins: Identification of novel IDO1 inhibitors.
  • 5
Heme Oxygenase-2 (HO-2) as a therapeutic target: Activators and inhibitors.
  • 15
Progress in the development of selective heme oxygenase-1 inhibitors and their potential therapeutic application.
  • 21
Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines.
  • 19
...
1
2
3
...

References

SHOWING 1-10 OF 63 REFERENCES
Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors.
  • 27
Novel imidazole derivatives as heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2) inhibitors and their cytotoxic activity in human-derived cancer cell lines.
  • 35
Structural insights into human heme oxygenase-1 inhibition by potent and selective azole-based compounds
  • 27
  • Highly Influential
  • PDF
Antitumor properties of substituted (αE)-α-(1H-indol-3-ylmethylene)benzeneacetic acids or amides.
  • 7
Evaluation of Imidazole‐Based Compounds as Heme Oxygenase‐1 Inhibitors
  • 24
A focus on heme oxygenase-1 (HO-1) inhibitors.
  • 53
Experimental and in silico characterization of a biologically active inosose
  • 9
...
1
2
3
4
5
...