1220904-65-3Relevant academic research and scientific papers
Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors
Zhang, Shu-Wei,Gong, Chao-Jun,Su, Ming-Bo,Chen, Fei,He, Ting,Zhang, Yang-Ming,Shen, Qian-Qian,Su, Yi,Ding, Jian,Li, Jia,Chen, Yi,Nan, Fa-Jun
, p. 804 - 815 (2020)
A series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors was developed during our previous work. In the present work, a new series of highly potent bisthiazole-based compounds were designed and synthesized. Among the prepared compounds, compound H13, which contains an α-(S)-methyl-substituted benzyl group, displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound H13 has a favorable PK profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model for colitis-associated colonic tumorigenesis.
ARYL-2,2'-TANDEM BISTHIAZOLE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0052; 0053, (2019/07/18)
The present invention relates to an aryl-2,2'-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2'-tandem bisthiazole compound with the structure as shown in general f
NOVEL SPIRO IMIDAZOLONES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE
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Page/Page column 200-201, (2011/10/13)
The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
