C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4)inhibitors, compound profiling in cell-based target engagement assays
Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between
Le Bihan, Yann-Va?,Lanigan, Rachel M.,Atrash, Butrus,McLaughlin, Mark G.,Velupillai, Srikannathasan,Malcolm, Andrew G.,England, Katherine S.,Ruda, Gian Filippo,Mok, N. Yi,Tumber, Anthony,Tomlin, Kathy,Saville, Harry,Shehu, Erald,McAndrew, Craig,Carmichael, LeAnne,Bennett, James M.,Jeganathan, Fiona,Eve, Paul,Donovan, Adam,Hayes, Angela,Wood, Francesca,Raynaud, Florence I.,Fedorov, Oleg,Brennan, Paul E.,Burke, Rosemary,van Montfort, Rob L.M.,Rossanese, Olivia W.,Blagg, Julian,Bavetsias, Vassilios
supporting information
p. 316 - 337
(2019/06/05)
Novel aminoethylbiphenyls as 5-HT7 receptor ligands
The synthesis of a series of aminoethylbiphenyls as novel 5-HT7 receptor ligands is described. The novel derivatives exhibit high affinity for the 5-HT7 receptor with selectivity toward 5-HT1A receptor.
Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors
A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen atom at the C-6 position. The best compounds are low nanomolar inhibitors of Src kinase, and have potent activity against Src-transformed fibroblast cells.
Berger, Dan,Dutia, Minu,Powell, Dennis,Wissner, Allan,DeMorin, Frenel,Raifeld, Yuri,Weber, Jennifer,Boschelli, Frank
p. 2989 - 2992
(2007/10/03)
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