The discovery and synthesis of novel adenosine substituted 2, 3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1)

PG Jagtap, GJ Southan, E Baloglu, S Ram…

文献索引：Jagtap, Prakash G.; Southan, Garry J.; Baloglu, Erkan; Ram, Siya; Mabley, Jon G.; Marton, Anita; Salzman, Andrew; Szabo, Csaba Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 1 p. 81 - 85

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被引用次数: 54

摘要

A series of novel 4-(N-acyl)-2, 3-dihydro-1H-isoindol-1-ones have been prepared from methyl-3-nitro-2-methylbenzoate and linked through various spacers to the adenosine derivatives 11 and 12. We found that potent inhibition of poly (ADP-ribose) polymerase-1 (PARP-1) was achieved when isoindolinone was linked to adenosine by a spacer group of a specific length. Introduction of piperazine and succinyl linkers between the isoindolinone ...