30609-21-3Relevant academic research and scientific papers
ALKOXYBENZALDEHYDE DERIVATIVES AND PRECURSORS THEREOF
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Page/Page column 12; 14-15, (2020/05/29)
The present invention refers to alkoxybenzaldehyde derivatives and precursors thereof. The invention further refers to perfume compositions and fragranced article comprising them.
Discovery and optimization of novel N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities
Hu, Qingqing,Wang, Chao,Xiang, Qiuping,Wang, Rui,Zhang, Cheng,Zhang, Maofeng,Xue, Xiaoqian,Luo, Guolong,Liu, Xiaomin,Wu, Xishan,Zhang, Yan,Wu, Donghai,Xu, Yong
, (2019/12/26)
Tripartite motif-containing protein 24 (TRIM24), recognized as an epigenetic reader for acetylated H3K23 (H3K23ac) via its bromodomain, has been closely involved in tumorigenesis or tumor progression of several cancers. Developing inhibitors of TRIM24 is significant for functional studies and drug discovery. Herein, we report the identification, optimization and evaluation of N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amines as TRIM24 bromodomain inhibitors starting from an in house library screening. Structure-based optimization leads to two potent and selective compounds 11d and 11h in an Alphascreen assay with IC50 values of 1.88 μM and 2.53 μM, respectively. The viability assay demonstrates the great potential of this series of compounds as inhibitors of proliferation of prostate cancer (PC) cells LNCaP, C4-2B. A colony formation assay further supports this inhibitory activity. Compounds 11d and 11h inhibit cell proliferation of other cancer types such as non-small cell lung cancer (NSCLC) cells A549 with IC50 values of 1.08 μM and 0.75 μM, respectively. These data suggests that compounds 11d and 11h are promising lead compounds for further research.
Nitrogen containing heterocyclic compounds
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, (2008/06/13)
Compounds of the formula (III): STR1 or salts or acyl derivatives thereof, for use as antifungal and antiprotozoal agents are disclosed. Compositions containing the compounds are also disclosed as are method for the preparation of the compounds and interm
Design of Inhibitors from the Three-Dimensional Structure of Alcohol Dehydrogenase. Chemical Synthesis and Enzymatic Properties
Freudenreich, Charles,Samama, Jean-Pierre,Biellmann, Jean-Francois
, p. 3344 - 3353 (2007/10/02)
Inhibitors of liver alcohol dehydrogenase were designed from the three-dimensional structure of the enzyme.The ligand to the catalytic zinc ion is an amide group or, better, a formamide group.With the latter function, a hydrogen bond between the NH group and the hydroxyl group of Ser-48 may be formed.The hydrophobic substrate binding site brings structural restraints. α-ω bifunctional molecules show good inhibitory properties possibly due to the interactions with polar residues at the entrance of the substrate binding site.
