Document Type
Article
Publication Date
3-1-2014
Publication Title
Bioorganic & Medicinal Chemistry Letters
Abstract
The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy.
Recommended Citation
Zhong, Bo; Lama, Rati; Ketchart, Wannarasmi; Montano, Monica M.; and Su, Bin, "Lead Optimization of HMBA to Develop Potent HEXIM1 Inducers" (2014). Chemistry Faculty Publications. 401.
https://engagedscholarship.csuohio.edu/scichem_facpub/401
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.2014.01.025
Version
Postprint
Volume
24
Issue
5
Comments
This work was supported by Center for Gene Regulation in Health and Disease (GRHD) of Cleveland State University and Ohio Department of Development (ODOD) to B.S. and NIH grant CA092440 to M.M.M.