Copalic acid analogs down-regulate androgen receptor and inhibit small chaperone protein.
Basic Information
ID: ALA4024729
Journal: Bioorg Med Chem Lett
Title: Copalic acid analogs down-regulate androgen receptor and inhibit small chaperone protein.
Authors: Idippily ND, Zheng Q, Gan C, Quamine A, Ashcraft MM, Zhong B, Su B.
Abstract: Copalic acid, one of the diterpenoid acids in copaiba oil, inhibited the chaperone function of α-crystallin and heat shock protein 27kD (HSP27). It also showed potent activity in decreasing an HSP27 client protein, androgen receptor (AR), which makes it useful in prostate cancer treatment or prevention. To develop potent drug candidates to decrease the AR level in prostate cancer cells, more copalic acid analogs were synthesized. Using the level of AR as the readout, 15 of the copalic acid analogs were screened and two compounds were much more potent than copalic acid. The compounds also dose-dependently inhibited AR positive prostate cancer cell growth. Furthermore, they inhibited the chaperone activity of α-crystallin as well.
CiteXplore: 28442254
DOI: 10.1016/j.bmcl.2017.04.046
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