1338320-90-3Relevant academic research and scientific papers
Synthesis and biological evaluation of 1-arylsulfonyl-5-(N -hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo
Lai, Mei-Jung,Huang, Han-Li,Pan, Shiow-Lin,Liu, Yi-Min,Peng, Chieh-Yu,Lee, Hsueh-Yun,Yeh, Teng-Kuang,Huang, Po-Hsien,Teng, Che-Ming,Chen, Ching-Shih,Chuang, Hsun-Yueh,Liou, Jing-Ping
, p. 3777 - 3791 (2012/07/27)
A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI50 values ranging from 0.36 to 1.21 μM against Hep3B, MDA-MB-231, PC-3, and A549 human cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with IC 50 values of 12.3, 4.0, 1.0 nM, respectively, which are comparable to 1. In in vivo efficacy evaluation against lung A549 xenograft model, 8 displayed better antitumor activity than compound 1.
INDOLYL OR INDOLINYL HYDROXAMATE COMPOUNDS
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Page/Page column 8; 9, (2011/10/13)
Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
