245126-04-9Relevant academic research and scientific papers
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3,4- tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N- methyltransferase versus the α2-adrenoceptor
Grunewald, Gary L.,Caldwell, Timothy M.,Li, Qifang,Criscione, Kevin R.
, p. 3315 - 3323 (1999)
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated as inhibitors of phenylethanolamine N- methyltransferase (PNMT) and as inhibitors of the binding of clonidine at the α2-adrenoceptor. These compounds we
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 201, (2017/08/01)
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity
Grunewald, Gary L.,Lu, Jian,Criscione, Kevin R.,Okoro, Cosmas O.
, p. 5319 - 5323 (2007/10/03)
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the α2-adrenoceptor. Although their PNMT inhibitory potency decreased compared with corresponding 3-methyl-, 3-hydroxymethyl- or 3-unsubstituted-THIQs, some of them showed good selectivity due to their extremely low α2-adrenoceptor affinity.
