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From Far West to East: Joining the Molecular Architecture of Imidazole-like Ligands in HO-1 Complexes. | LitMetric

AI Article Synopsis

  • HO-1 overexpression is linked to various human cancers, often resulting in poor clinical outcomes, making it a target for anticancer therapies.
  • Researchers used a fragment-based approach to create and screen 1,000 novel compounds as potential HO-1 inhibitors, ultimately identifying a new series of indole-based compounds.
  • Among the synthesized compounds, one demonstrated a promising inhibitory capacity with an IC of 1.03 μM, indicating the approach's success and potential for further development.

Article Abstract

HO-1 overexpression has been reported in several cases/types of human malignancies. Unfortunately, poor clinical outcomes are reported in most of these cases, and the inhibition of HO-1 is considered a valuable and proven anticancer approach. To identify novel hit compounds suitable as HO-1 inhibitors, we report here a fragment-based approach where ligand joining experiments were used. The two most important parts of the classical structure of the HO-1 inhibitors were used as a starting point, and 1000 novel compounds were generated and then virtually evaluated by structure and ligand-based approaches. The joining experiments led us to a novel series of indole-based compounds. A synthetic pathway for eight selected molecules was designed, and the compounds were synthesized. The biological activity revealed that some molecules reach the micromolar activity, whereas molecule inhibits the HO-1 with an IC of 1.03 μM. This study suggested that our joining approach was successful, and a novel hit compound was generated. These results are ongoing for further development.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8704944PMC
http://dx.doi.org/10.3390/ph14121289DOI Listing

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