Synthesis and Biological Evaluation of Novel Sulfonanilide Compounds as Antiproliferative Agents for Breast Cancer
Document Type
Article
Publication Date
5-1-2008
Publication Title
Journal of Combinatorial Chemistry
Abstract
Combinatorial chemistry approaches facilitate drug discovery processes and result in structural modifications of lead compounds that enhance pharmacological activity, improve pharmacokinetic properties, or reduce unwanted side effects. Epidemiological and animal model studies have suggested that nonsteroidal anti-inflammatory drugs (NSAIDs) can act as chemopreventive agents. The cyclooxygenase-2 (COX-2) inhibitor nimesulide shows anticancer effects in several cancer cell lines via COX-2-dependent and -independent mechanisms. The molecular structure of nimesulide was used as a starting scaffold to design novel sulfonanilide analogs and examine the structural features that contribute to this anticancer effect. A systematic combinatorial chemical approach was used to generate diversely substituted sulfonanilide derivatives that were tested for their effects on the proliferation of human breast cancer cells. Structure–function analysis indicated that the inhibition of cell growth by compounds derived from the novel sulfonanilides required a bulky terminal phenyl ring, a methanesulfonamide, and a hydrophobic carboxamide moiety.
Recommended Citation
Su, Bin; Darby, Michael V.; and Brueggemeier, Robert W., "Synthesis and Biological Evaluation of Novel Sulfonanilide Compounds as Antiproliferative Agents for Breast Cancer" (2008). Chemistry Faculty Publications. 451.
https://engagedscholarship.csuohio.edu/scichem_facpub/451
DOI
10.1021/cc700138n
Volume
10
Issue
3
Comments
This work was supported by the National Institutes of Health (NIH) Grant R01 CA73698 (R.W.B.), the USAMRMC Breast Cancer Program Grant W81XWH-08-1-0521, and The Ohio State University Comprehensive Cancer Center Breast Cancer Research Fund.