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Bioorg Med Chem Lett ; 18(14): 3942-5, 2008 Jul 15.
Article in English | MEDLINE | ID: mdl-18579376

ABSTRACT

We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors.


Subject(s)
Enzyme Inhibitors/pharmacology , Poly(ADP-ribose) Polymerase Inhibitors , Chemistry, Pharmaceutical , Drug Design , Enzyme Inhibitors/chemistry , HeLa Cells , Humans , Hydrogen Bonding , Inhibitory Concentration 50 , Models, Chemical , Molecular Conformation , Molecular Structure , Poly (ADP-Ribose) Polymerase-1 , Poly(ADP-ribose) Polymerases/chemistry , Structure-Activity Relationship , Substrate Specificity
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