INHIBITORS OF HEXOKINASE AND METHODS OF USE THEREOF
Provided herein are substituted substituted heterocycles useful as inhibitors of the HKII enzyme. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention further provides medical uses of substituted heterocycles, for example, as antitumor agents.
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Page/Page column 142
(2018/09/25)
INHIBITORS OF HEXOKINASE AND METHODS OF USE THEREOF
Provided herein are substituted fused oxazoline derivatives and substituted pyran derivatives useful as inhibitors of the HKII enzyme. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention further provides medical uses of substituted fused oxazoline derivatives and substituted pyran derivatives, for example, as antitumor agents.
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Page/Page column 101
(2017/04/04)
Discovery of N-(4′-(indol-2-yl)phenyl)sulfonamides as novel inhibitors of HCV replication
A series of novel 2-phenylindole analogs were synthesized and evaluated for activity in subgenomic HCV replicon inhibition assays. Several compounds containing small alkyl sulfonamides on the phenyl ring exhibiting submicromolar EC50 values against the genotype 1b replicon were identified. Among these, compound 25d potently inhibited the 1b replicon (EC50 = 0.17 μM) with 147-fold selectivity with respect to cytotoxicity. Compound 25d was stable in the presence of human liver microsomes and had a good pharmacokinetic profile in rats with an IV half-life of 4.3 h and oral bioavailability (F) of 58%.
Chen, Guangming,Ren, Hongyu,Turpoff, Anthony,Arefolov, Alexander,Wilde, Richard,Takasugi, James,Khan, Atiyya,Almstead, Neil,Gu, Zhengxian,Komatsu, Takashi,Freund, Connie,Breslin, Jamie,Colacino, Joseph,Hedrick, Jean,Weetall, Marla,Karp, Gary M.
p. 3942 - 3946
(2013/07/27)
Methods and compounds for treating proliferative diseases
The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).
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(2008/06/13)
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