| Literature DB >> 27344487 |
Hsueh-Yun Lee1, Chih-Yi Chang1, Chih-Jou Su2, Han-Li Huang2, Samir Mehndiratta1, Yuh-Hsuan Chao1, Chia-Ming Hsu2, Sunil Kumar1, Ting-Yi Sung2, Yi-Zhen Huang2, Yu-Hsuan Li1, Chia-Ron Yang3, Jing-Ping Liou4.
Abstract
This study reports the design and synthesis of 2-(phenylsulfonyl)quinoline N-hydroxyacrylamides (8a-k). Structure-activity relationship studies focusing on regio-effect of N-hydroxyacrylamide moiety and influence of the sulfonyl linker revealed that N-hydroxy-3-[3-(quinoline-2-sulfonyl)-phenyl]-acrylamide (8f) showed remarkable enzymatic and cellular activity. The GI50 values of 8f for HL-60, HCT116, PC-3, and A549 cells were found to be 0.29, 0.08, 0.15, and 0.27 μM, respectively. The compounds are therefore more potent than FDA approved PXD-101 and SAHA. They also have an effect on the acetylation degree of histone H3 and α-tubulin. In in vivo studies, 8f showed marked inhibition of the growth of HCT116 xenografts.Entities:
Keywords: 2-(Phenylsulfonyl)quinoline; Anticancer agents; Histone deacetylase inhibitors
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Year: 2016 PMID： 27344487 DOI： 10.1016/j.ejmech.2016.06.023
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514