305863-15-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of O-alkyl umbelliferone derivatives as pancreatic lipase inhibitors
Yadav, Nisha,Auti, Prashant,George, Ginson,Paul, Atish T.
, p. 1265 - 1271 (2020/12/04)
A series of coumarin derivatives were synthesised through O-alkylation of umbelliferone. These derivatives were screened for their pancreatic lipase (PL) inhibitory potential. The PL inhibitory effect of compounds with various benzyl and long chain alkyl substituents on umbelliferone were analysed. The compound 1g, having the geranyl substituent was found to have better PL inhibitory potential with an IC50 of 21.64 M. The compounds 1a-j were subjected to molecular docking into the crystal structure of human PL. The molecular docking results are in correlation with the in vitro PL inhibition activity, wherein compound 1g showed a higher MolDock score of -122.12 kcal/mol. The long chain alkyl groups were found to have PL inhibition due to additional interactions with lid domain amino acids (Phe215, Tyr114, Phe77), as revealed by molecular docking study.
HDAC8 INHIBITORS FOR TREATING CANCER
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Paragraph 0271; 0272, (2015/03/13)
Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.
Synthesis and Biological Evaluation of ortho-Aryl N-Hydroxycinnamides as Potent Histone Deacetylase (HDAC) 8 Isoform-Selective Inhibitors
Huang, Wei-Jan,Wang, Yi-Ching,Chao, Shi-Wei,Yang, Chen-Yui,Chen, Liang-Chieh,Lin, Mei-Hsiang,Hou, Wen-Chi,Chen, Mei-Yu,Lee, Tai-Lin,Yang, Ping,Chang, Chung-I
, p. 1815 - 1824 (2012/10/29)
Histone deacetylases (HDACs) are a family of enzymes that play a crucial role in biological process and diseases. In contrast to other isozymes, HDAC8 is uniquely incapable of histone acetylation. In order to delineate its physiological function, we devel
