Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 591-11-7, Name is 5-Methylfuran-2(5H)-one, molecular formula is , belongs to benzofurans compound. In a document, author is Chen, Xiuli, Computed Properties of C5H6O2.
Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity
SIRT6 activation is thought to be a promising target for the treatment of many diseases, particularly cancer. Herein, we report the discovery of a series of new small-molecule SIRT6 activators. Structure-activity relationship analyses led to the identification of the most potent compound, 2-(1-benzofuran-2-yl)-N-(diphenylmethyl) quinoline-4-carboxamide (12q), which showed an EC1.5 value of 0.58 +/- 0.12 mu M and an EC50 value of 5.35 +/- 0.69 mu M against SIRT6-dependent peptide deacetylation in FLUOR DE LYS assay. It exhibited weak or no activity against other HDAC family members as well as 415 kinases, indicating good selectivity for SIRT6. 12q significantly inhibited the proliferation and migration of pancreatic ductal adenocarcinoma (PDAC) cells in vitro. It also markedly suppressed the tumor growth in a PDAC tumor xenograft model. This compound showed attractive pharmacokinetic properties. Overall, 12q could be a good lead compound for the treatment of PDAC, and it is worthy of further study.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem