Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2
摘要:
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner. H-1 NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme. (C) 2008 Elsevier Ltd. All rights reserved.
Arylmethylenyl derivatives of thiazolidnones, imidazolidinones and oxazolidinones useful as antiallergy agents and antiinflamatory agents
申请人:WARNER-LAMBERT COMPANY
公开号:EP0343643A2
公开(公告)日:1989-11-29
The present invention is for selected novel compounds, as well as, pharmaceutical compositions and methods of use for known and the selected novel compounds both of the formula
having activity useful for treating allergies and inflammation.
Thiazolidinone derivatives as hypoglycemic agents and for treating Alzheimer's disease
申请人:ELI LILLY AND COMPANY
公开号:EP0587377A2
公开(公告)日:1994-03-16
Provided are methods for treating hyperglycemia and Alzheimer's disease utilizing certain rhodanine derivatives. Certain of the rhodanine derivatives utilized in the instant methods are novel and, accordingly, such compounds, process for preparing same and pharmaceutical formulations thereof, are also provided.
Compounds useful as hypoglycemic agents and for treating Alzheimer's disease
申请人:ELI LILLY AND COMPANY
公开号:EP0915090A1
公开(公告)日:1999-05-12
Provided are methods for treating hyperglycemia and Alzheimer's disease utilizing certain rhodanine derivatives. Certain of the rhodanine derivatives utilized in the instant methods are novel and, accordingly, such compounds, process for preparing same and pharmaceutical formulations thereof, are also provided.