Structure−Activity Relationship Studies of a Series of Novel δ-Lactam-Based Histone Deacetylase Inhibitors
| Autor: | Bum Woo Park, Ky-Youb Nam, Kiho Lee, Chang Woo Lee, Hee Yoon Lee, Jong Soon Kang, Jung Whan Han, Yongseok Choi, Shanthaveerappa K. Boovanahalli, Eun Hyun Choi, Tae-Gyu Chun, Hwan Mook Kim, Dong-Kyu Ryu, Sang Bae Han, Song-Kyu Park, Moo Rim Kang, Gyoonhee Han |
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| Rok vydání: | 2007 |
| Předmět: |
Lipopolysaccharides
Models Molecular Lactams medicine.drug_class Transplantation Heterologous Antineoplastic Agents Nitric Oxide Cell Line Proinflammatory cytokine Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Cell Line Tumor Drug Discovery medicine Animals Humans Hydroxamic acid biology Tumor Necrosis Factor-alpha Chemistry Cell growth Anti-Inflammatory Agents Non-Steroidal Histone deacetylase inhibitor Histone Deacetylase Inhibitors Biochemistry Enzyme inhibitor Cell culture biology.protein Molecular Medicine Histone deacetylase Drug Screening Assays Antitumor |
| Zdroj: | Journal of Medicinal Chemistry. 50:2737-2741 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm0613828 |
| Popis: | We synthesized a series of delta-lactam-based HDAC inhibitors that were identified with various degrees of anti-inflammatory and cell growth inhibitory activities. Compounds possessing significant HDAC inhibitory activity exhibited both anti-inflammatory and cell growth inhibitory activities as well as significant tumor growth inhibition in the in vivo tumor xenograft experiments. Besides, these compounds demonstrated anti-inflammatory properties in vitro via suppression of the production of the proinflammatory cytokine TNF-alpha and nitric oxide by LPS-stimulated RAW264.7 cells. |
| Databáze: | OpenAIRE |
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