Document Type
Article
Publication Date
6-1-2017
Publication Title
Bioorganic and Medicinal Chemistry Letters
Abstract
Copalic acid, one of the diterpenoid acids in copaiba oil, inhibited the chaperone function of α-crystallin and heat shock protein 27 kD (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.
Recommended Citation
Idippily, Nethrie D.; Zheng, Qiaoyun; Gan, Chunfang; Quamine, Aicha; Ashcraft, Morgan M.; Zhong, Bo; and Su, Bin Ph.D., "Copalic Acid Analogs Down-regulate Androgen Receptor and Inhibit Small Chaperone Protein" (2017). Chemistry Faculty Publications. 519.
https://engagedscholarship.csuohio.edu/scichem_facpub/519
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-No Derivative Works 4.0 International License.
DOI
10.1016/j.bmcl.2017.04.046
Version
Postprint
Volume
27
Issue
11
Comments
This work was supported by Center for Gene Regulation in Health and Disease (GRHD) and summer undergraduate research program of Cleveland State University. Aicha Quamine was supported by McNair scholarship.