352704-97-3Relevant articles and documents
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
Lin, Hong,Yamashita, Dennis S.,Zeng, Jin,Xie, Ren,Wang, Wenyong,Nidarmarthy, Sirishkumar,Luengo, Juan I.,Rhodes, Nelson,Knick, Victoria B.,Choudhry, Anthony E.,Lai, Zhihong,Minthorn, Elisabeth A.,Strum, Susan L.,Wood, Edgar R.,Elkins, Patricia A.,Concha, Nestor O.,Heerding, Dirk A.
scheme or table, p. 673 - 678 (2010/07/05)
2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.
Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-aminoethoxy)pyridine as novel nicotinic receptor ligands
Lin, Nan-Horng,Dong, Liming,Bunnelle, William H,Anderson, David J,Meyer, Michael D
, p. 3321 - 3324 (2007/10/03)
Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5′ and 6′-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [3H](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited Ki values ranging from 0.076 to 319 nM compared to a Ki value of 26 nM for compound 1. Among the compounds tested, 5′-vinyl-6′-chloro substituted 1 was the most potent.
