Author/Authors :
George S. Sheppard، نويسنده , , Jieyi Wang، نويسنده , , Megumi Kawai، نويسنده , , Nwe Y. BaMaung، نويسنده , , Richard A. Craig، نويسنده , , Scott A. Erickson، نويسنده , , Linda Lynch، نويسنده , , Jyoti Patel، نويسنده , , Fan Yang، نويسنده , , Xenia B. Searle، نويسنده , , Pingping Lou، نويسنده , , Chang Park، نويسنده , , Ki H. Kim، نويسنده , , Jack Henkin، نويسنده , , Richard Lesniewski، نويسنده ,
Abstract :
Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).
