1310356-22-9Relevant academic research and scientific papers
The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors
Xiang, Yibin,Hirth, Bradford,Asmussen, Gary,Biemann, Hans-Peter,Bishop, Kimberly A.,Good, Andrew,Fitzgerald, Maria,Gladysheva, Tatiana,Jain, Annuradha,Jancsics, Katherine,Liu, Jinyu,Metz, Markus,Papoulis, Andrew,Skerlj, Renato,Stepp, J. David,Wei, Ronnie R.
, p. 3050 - 3056 (2011)
Novel benzofuran-2-carboxylic acids, exemplified by 29, 38 and 39, have been discovered as potent Pim-1 inhibitors using fragment based screening followed by X-ray structure guided medicinal chemistry optimization. The compounds demonstrate potent inhibition against Pim-1 and Pim-2 in enzyme assays. Compound 29 has been tested in the Ambit 442 kinase panel and demonstrates good selectivity for the Pim kinase family. X-ray structures of the inhibitor/Pim-1 binding complex reveal important salt-bridge and hydrogen bond interactions mediated by the compound's carboxylic acid and amino groups.
