Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.
Article Details
- CitationCopy to clipboard
Kikuchi K, Hibi S, Yoshimura H, Tai K, Hida T, Tokuhara N, Yamauchi T, Nagai M
Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.
Bioorg Med Chem Lett. 2000 Apr 3;10(7):619-22.
- PubMed ID
- 10762038 [ View in PubMed]
- Abstract
We have designed and synthesized a series of pyrazole derivatives as candidate retinoic acid receptor (RAR) agonists. One of them, 4-[5-(1, 5-diisopropyl-1H-3-pyrazolyl)-1H-2-pyrrolyl]benzoic acid (11b), which possesses a 2,5-disubstituted pyrrole moiety, showed selective transactivation activity for the RAR alpha receptor, and had highly potent cell-differentiating activity on HL-60 cells.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Tretinoin Retinoic acid receptor alpha IC 50 (nM) 0.78 N/A N/A Details Tretinoin Retinoic acid receptor beta IC 50 (nM) 0.9 N/A N/A Details Tretinoin Retinoic acid receptor gamma IC 50 (nM) 0.5 N/A N/A Details