491837-75-3Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of a series of benzo[ de ][1,7]naphthyridin-7(8 H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors
Ye, Na,Chen, Chuan-Huizi,Chen, Tiantian,Song, Zilan,He, Jin-Xue,Huan, Xia-Juan,Song, Shan-Shan,Liu, Qiufeng,Chen, Yi,Ding, Jian,Xu, Yechun,Miao, Ze-Hong,Zhang, Ao
, p. 2885 - 2903 (2013/06/04)
A series of benzo[de][1,7]naphthyridin-7(8H)-ones possessing a functionalized long-chain appendage have been designed and evaluated as novel PARP1 inhibitors. The initial effort led to the first-generation PARP1 inhibitor 26 bearing a terminal phthalazin-
From tyrosine to glycine: Synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor
Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cara, Carlota Lopez,Preti, Delia,Cruz-Lopez, Olga,Tabrizi, Mojgan Aghazadeh,Moorman, Allan R.,Gessi, Stefania,Fogli, Eleonora,Sacchetto, Valeria,Borea, Pier Andrea
, p. 3706 - 3715 (2008/02/09)
The characterization of the native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtype-selective antagonists with a "druglike" profile. However, a tyrosine derivative named KN-62 exhibits selective P2Xsub
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
Steinhagen, Henning,Gerisch, Michael,Mittendorf, Joachim,Schlemmer, Karl-Heinz,Albrecht, Barbara
, p. 3187 - 3190 (2007/10/03)
A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC50=2 μM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (ICsu
