89469-44-3Relevant academic research and scientific papers
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: Effect of sulfonamides P3 substituents on potency and selectivity
Ayesa, Susana,Lindquist, Charlotta,Agback, Tatiana,Benkestock, Kurt,Classon, Bjoern,Henderson, Ian,Hewitt, Ellen,Jansson, Katarina,Kallin, Anders,Sheppard, Dave,Samuelsson, Bertil
experimental part, p. 1307 - 1324 (2009/08/08)
Highly potent and selective 4-amidofuran-3-one inhibitors of cathepsin S are described. The synthesis and structure-activity relationship of a series of inhibitors with a sulfonamide moiety in the P3 position is presented. Several members of the series show sub-nanomolar inhibition of the target enzyme as well as an excellent selectivity profile and good cellular potency. Molecular modeling of the most interesting inhibitors describes interactions in the extended S3 pocket and explains the observed selectivity towards cathepsin K.
Synthesis and crystallographic studies of new acridinic esters and amides: An efficient synthetic route to 4-methyl functionalized acridines
Chiron, Julien,Galy, Jean-Pierre
, p. 1653 - 1672 (2007/10/03)
In order to open a new way in antitumor drugs research, an efficient synthetic route to mono functional 4-substitued acridine derivatives has been developed on the basis of direct electrophilic substitution of acridine. This method leads to a wide range of simple acridinic patterns that can be linked to various side chains. We present here the synthesis of two new families of acridine ester and amide derivatives, obtained from acridinic alcohol and amine respectively, with high yields. Some crystallographic aspects of one representative compound of each family are discussed.
