39478-93-8Relevant articles and documents
Design, synthesis and activity of bisubstrate, transition-state analogues and competitive inhibitors of aspartate transcarbamylase
Grison, Claude,Coutrot, Philippe,Comoy, Corinne,Balas, Laurence,Joliez, Stephane,Lavecchia, Guido,Oliger, Patrick,Penverne, Bernadette,Serre, Valerie,Herve, Guy
, p. 333 - 344 (2007/10/03)
Aspartate transcarbamylase initiates the de novo biosynthetic pathway for the production of the pyrimidine nucleotides, precursors of nucleic acids. This pathway is particularly active in rapidly growing cells and tissues. Thus, this enzyme has been tested as a potential target for antiproliferative drugs. In the present work, on the basis of its structural and mechanistic properties, a series of substrate analogues, including potential suicide-pseudosubstrates was synthesized and their putative inhibitory effects were tested using E. coli aspartate transcarbamylase as a model. Two of these compounds appear to be very efficient inhibitors of this enzyme.
SYNTHESIS OF ALKYLATED METHYLENE BISPHOSPHONATES VIA ORGANOTHALLIUM INTERMEDIATES
Hutchinson, David W.,Semple, Graeme
, p. 145 - 152 (2007/10/02)
Thallium(I) derivatives of esterified methylene bisphosphonates can be readily obtained by treating the latter with thallium(I) ethoxide under anhydrous conditions.Alkylation of the thallium(I) derivatives by a range of primary alkyl iodides takes place smoothly, and significantly higher yields are obtained than for the corresponding reactions with lithio or sodio derivatives.