Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC
作者:Yannick Rose、Stéphane Ciblat、Ranga Reddy、Adam C. Belley、Evelyne Dietrich、Dario Lehoux、Geoffrey A. McKay、Hugo Poirier、Adel Rafai Far、Daniel Delorme
DOI:10.1016/j.bmcl.2005.11.009
日期:2006.2
The preparation and biological evaluation of 5-substituted-6-hydroxy-2-(anilino)pyrimidinones as a new class of DNA polymerase IIIC inhibitors, required for the replication of chromosomal DNA in Gram-positive bacteria, are described. These new dGTP competitive inhibitors displayed good levels of in vitro inhibition and antibacterial activity against Staphylococcus aureus. A new class of dATP competitive inhibitors, 6-substituted-2-amino-5-alkyl-pyrimidin-4-ones, whose antibacterial activity was unaffected by serum, were identified. (c) 2005 Elsevier Ltd. All rights reserved.
PLATINUM COMPOUNDS FOR TREATING CELL PROLIFERATIVE DISEASE, PREPARATION METHODS AND USES THEREOF
PLATINUM COMPOUNDS FOR TREATING CELL PROLIFERATIVE DISEASES, PREPARATION METHOD AND USE THEREOF
申请人:Chen Xiaoping
公开号:US20140142079A1
公开(公告)日:2014-05-22
Disclosed are a class of platinum compounds with a leaving group of malonic acid derivatives containing amino and alkylamino, their pharmaceutically acceptable salts, their preparation methods and pharmaceutical composites comprising them. Disclosed also are for the uses of the compounds in the treatment of cell proliferative diseases, particularly for the treatment of cancers. The present platinum compounds have high water solubility and low toxicity.