905970-82-3Relevant academic research and scientific papers
Structure-activity relationship studies of a series of novel δ-lactam-based histone deacetylase inhibitors
Hwan, Mook Kim,Ryu, Dong-Kyu,Choi, Yongseok,Bum, Woo Park,Lee, Kiho,Sang, Bae Han,Lee, Chang-Woo,Kang, Moo-Rim,Jong, Soon Kang,Boovanahalli, Shanthaveerappa K.,Park, Song-Kyu,Jung, Whan Han,Chun, Tae-Gyu,Lee, Hee-Yoon,Nam, Ky-Youb,Eun, Hyun Choi,Han, Gyoonhee
, p. 2737 - 2741 (2008/02/04)
We synthesized a series of δ-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 antiinflammatory properties in vitro via suppression of the production of the proinflammatory cytokine TNF-α and nitric oxide by LPS-stimulated RAW264.7 cells.
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors
Kim, Hwan Mook,Lee, Kiho,Park, Bum Woo,Ryu, Dong Kyu,Kim, Kangjeon,Lee, Chang Woo,Park, Song-Kyu,Han, Jung Whan,Lee, Hee Yoon,Lee, Hyun Yong,Han, Gyoonhee
, p. 4068 - 4070 (2007/10/03)
δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.
