| 17827005 |
Anandan SK, Ward JS, Brokx RD, Denny T, Bray MR, Patel DV, Xiao XY: Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5995-9. Epub 2007 Aug 19.
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. |
2(0,0,0,2) |