Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365550 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
We have designed and synthesized a series of structurally novel hydroxamic acid-based histone deacetylase (HDAC) inhibitors characterized by a zinc chelating head group attached directly to a thiazole ring. The thiazole ring connects to a piperazine spacer, which is capped with a sulfonamide group. These novel molecules potently inhibit an HDAC enzyme mixture derived from HeLa cervical carcinoma cells and show potent antiproliferative activity against the breast cancer cell line MCF7.
Graphical abstractThe synthesis, histone deacetylase (HDAC) inhibitory activity and the antiproliferative activity of thiazole-5-hydroxamic acids 6–9 are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sampath-Kumar Anandan, John S. Ward, Richard D. Brokx, Trisha Denny, Mark R. Bray, Dinesh V. Patel, Xiao-Yi Xiao,