Literature DB >> 10762038

Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.

K Kikuchi1, S Hibi, H Yoshimura, K Tai, T Hida, N Tokuhara, T Yamauchi, M Nagai.   

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.

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Year:  2000        PMID: 10762038     DOI: 10.1016/s0960-894x(00)00066-4

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Probing biological activity through structural modelling of ligand-receptor interactions of 2,4-disubstituted thiazole retinoids.

Authors:  Hesham Haffez; David R Chisholm; Natalie J Tatum; Roy Valentine; Christopher Redfern; Ehmke Pohl; Andrew Whiting; Stefan Przyborski
Journal:  Bioorg Med Chem       Date:  2018-02-10       Impact factor: 3.641

  1 in total

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