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Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo.
Lai MJ, Huang HL, Pan SL, Liu YM, Peng CY, Lee HY, Yeh TK, Huang PH, Teng CM, Chen CS, Chuang HY, Liou JP. Lai MJ, et al. Among authors: Huang HL, Huang PH. J Med Chem. 2012 Apr 26;55(8):3777-91. doi: 10.1021/jm300197a. Epub 2012 Apr 5. J Med Chem. 2012. PMID: 22439863 Free PMC article.
Phenyl Benzenesulfonylhydrazides Exhibit Selective Indoleamine 2,3-Dioxygenase Inhibition with Potent in Vivo Pharmacodynamic Activity and Antitumor Efficacy.
Lin SY, Yeh TK, Kuo CC, Song JS, Cheng MF, Liao FY, Chao MW, Huang HL, Chen YL, Yang CY, Wu MH, Hsieh CL, Hsiao W, Peng YH, Wu JS, Lin LM, Sun M, Chao YS, Shih C, Wu SY, Pan SL, Hung MS, Ueng SH. Lin SY, et al. Among authors: Huang HL. J Med Chem. 2016 Jan 14;59(1):419-30. doi: 10.1021/acs.jmedchem.5b01640. Epub 2015 Dec 23. J Med Chem. 2016. PMID: 26653033
2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase.
Lee HY, Chang CY, Su CJ, Huang HL, Mehndiratta S, Chao YH, Hsu CM, Kumar S, Sung TY, Huang YZ, Li YH, Yang CR, Liou JP. Lee HY, et al. Among authors: Huang HL, Huang YZ. Eur J Med Chem. 2016 Oct 21;122:92-101. doi: 10.1016/j.ejmech.2016.06.023. Epub 2016 Jun 16. Eur J Med Chem. 2016. PMID: 27344487
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. ...
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 compo …
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