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Design, synthesis, and evaluation of cyclic amide/imide-bearing hydroxamic acid derivatives as class-selective histone deacetylase (HDAC) inhibitors.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Shinji, Chihiro Satoko Imai, Keisuke Yoshida, Minoru Hashimoto, Yuichi Miyachi, Hiroyuki |
| Copyright Year | 2006 |
| Abstract | A series of hydroxamic acid derivatives bearing a cyclic amide/imide group as a linker and/or cap structure, prepared during our structural development studies based on thalidomide, showed class-selective potent histone deacetylase (HDAC)-inhibitory activity. Structure-activity relationship studies indicated that the steric character of the substituent introduced at the cyclic amide/imide nitrogen atom, the presence of the amide/imide carbonyl group, the hydroxamic acid structure, the shape of the linking group, and the distance between the zinc-binding hydroxamic acid group and the cap structure are all important for HDAC-inhibitory activity and class selectivity. A representative compound (30w) showed potent p21 promoter activity, comparable with that of trichostatin A (TSA), and its cytostatic activity against cells of the human prostate cell line LNCaP was more potent than that of the well-known HDAC inhibitor, suberoylanilide hydroxamic acid (SAHA). |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/j.bmc.2006.07.008 |
| Alternate Webpage(s) | http://www.riken.jp/SPD/ChemicalGeneticsLab/Jounal/Shinji_C2006.pdf |
| PubMed reference number | 16877001 |
| Alternate Webpage(s) | https://doi.org/10.1016/j.bmc.2006.07.008 |
| Journal | Medline |
| Volume Number | 14 |
| Issue Number | 22 |
| Journal | Bioorganic & medicinal chemistry |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
