ArticleACS medicinal chemistry letters2013
Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
6 citing papers in PubMed, 20 citations in OpenAlex.
- Synthesis and Evaluation of Aromatic A-Ring 23-Oxavitamin DInternational journal of molecular sciences · 2025Article
- Clinical Research Progress of Small Molecule Compounds Targeting Nrf2 for Treating Inflammation-Related Diseases.Antioxidants (Basel, Switzerland) · 2022Review
- Hedgehog signaling pathway and vitamin D receptor gene variants as potential risk factors in odontogenic cystic lesions.Clinical oral investigations · 2019Article
- Design of Hedgehog pathway inhibitors for cancer treatment.Medicinal research reviews · 2019Review
- Probing seco-steroid inhibition of the hedgehog signaling pathway.Molecular and cellular biochemistry · 2019Article
- Targeted delivery of vitamin D3-loaded nanoparticles to C6 glioma cell line increased resistance to doxorubicin, epirubicin, and docetaxel in vitro.In vitro cellular & developmental biology. Animal · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
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Abstract
Previous structure-activity relationship studies for vitamin D3 (VD3) inhibition of Hedgehog (Hh) signaling directed the design, synthesis, and evaluation of a series of VD3-based analogues that contain an aromatic A-ring mimic. Characterization of these compounds in a series of cellular assays demonstrated their ability to potently and selectively down-regulate Hh pathway signaling. The most active of these, 17, inhibited pathway signaling in Hh-dependent mouse fibroblasts (IC50 = 0.74 ± 0.1 μM) and cultured cancer cells (IC50 values 3.8 ± 0.1 to 5.2 ± 0.2 μM). In addition, 17 demonstrated reduced activation of the vitamin D receptor (VDR) compared to VD3 in these cellular models. These results suggest that VD3-based analogues with an aromatic A-ring are a valid scaffold for the development of more selective and potent Hh pathway inhibitors and identify 17 as an intriguing lead from this class of compounds for further development. In addition, our analysis of Hh pathway inhibitors in cancer cells suggests that the murine basal cell carcinoma cell line ASZ001 and the human medulloblastoma cell line DAOY are appropriate in vitro cancer models for early stage evaluation of pathway inhibition.
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