120973-72-0Relevant academic research and scientific papers
2-Aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors
Mahboobi, Siavosh,Sellmer, Andreas,H?cher, Heymo,Garhammer, Christian,Pongratz, Herwig,Maier, Thomas,Ciossek, Thomas,Beckers, Thomas
, p. 4405 - 4418 (2008/02/13)
Histone deacetylase (HDAC) inhibitors are considered to be drugs for targeted cancer therapy and second-generation HDIs are currently being tested in clinical trials. Here, we report on the synthesis and biological evaluation of a novel HDAC inhibitor sca
Synthetic approaches to benzofuran containing Insulin Sensitivity Enhancer compounds for treatment of type II diabetes
Huff, Bret E.,Leffelman, Cindy L.,LeTourneau, Michael E.,Sullivan, Kevin A.,Ward, Jeffrey A.,Stille, John R.
, p. 1363 - 1384 (2007/10/03)
The search for Insulin Sensitivity Enhancer (ISE) compounds, for potential use in the treatment of Type II diabetes, has led to the synthesis of compounds that contain a benzofuran spacer between an aryloyl substituent and a 2,4-thiazolidinedione pharmacophore. Sequential combination of haloacetyl aryl substrates with 5-formylsalicylaldehyde gave the desired 2-aryloyl-5-formylbenzofuran intermediates. A related class of compounds, those with a methylene tether between the aromatic moiety and the benzofuran spacer, were also prepared through this strategy.
5-Formyl salicylaldehyde as a linker for the synthesis of benzofuran containing insulin sensitivity enhancer compounds
Stille, John R.,Ward, Jeffrey A.,Leffelman, Cindy,Sullivan, Kevin A.
, p. 9267 - 9270 (2007/10/03)
5-Formyl salicylaldehyde was prepared by treatment of 4-hydroxybenzaldehyde with HMTA in TFA. Reaction of this dialdehyde with α-haloacetyl aryl compounds gave 2,5-disubstituted benzofurans, from which an Insulin Sensitivity Enhancer compound was prepared.
Thiazolidinedione derivatives
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, (2008/06/13)
A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: A0 represents nitrogen or a moiety R1- , wherein, R1 represents hydrogen, alkyl or a substituted or unsubstituted aryl group;, R2 represents a moiety R3-Y-Z- wherein R3 represents substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl or a substituted or unsubstituted oxazolyl group, and Y represents -(CH2)n-wherein n represents zero or any integer in the range of 1 to 6 and Z represents -CH2-,-CH(OH)- or -CO-;, Raand Rbeach represent hydrogen or Raand Rbtogether represent a bond;, A represents a residue of a benzene ring, the carbon atoms of the residue having in total up to four substituents;, and X represents O or S; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of the compound and composition in medicine.
