Title compds. I [X = (un)substituted phenylene; Y = absent, CO, or CH2; R3 = absent, Ph, NH2, NHMe, etc.; R7 = H or halo; with provisions], and their pharmaceutically acceptable salts, are prepd. and disclosed as PARP inhibitors. Thus, e.g., II was prepd. by a multistep procedure (prepn. given). Select I were evaluated in PARP inhibition assays, e.g., II demonstrated an IC50 value of between >100 nM to <500 nM.
Preparation of azaindole derivatives for use as PARP inhibitors / G. Giannini, L. Vesci, S. Dallavalle, L. Merlini.
Preparation of azaindole derivatives for use as PARP inhibitors
S. DallavallePenultimo
;L. MerliniUltimo
2015
Abstract
Title compds. I [X = (un)substituted phenylene; Y = absent, CO, or CH2; R3 = absent, Ph, NH2, NHMe, etc.; R7 = H or halo; with provisions], and their pharmaceutically acceptable salts, are prepd. and disclosed as PARP inhibitors. Thus, e.g., II was prepd. by a multistep procedure (prepn. given). Select I were evaluated in PARP inhibition assays, e.g., II demonstrated an IC50 value of between >100 nM to <500 nM.
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