Design, synthesis, and biological evaluation of substituted 2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamine related compounds as fructose-1,6-bisphosphatase inhibitors.
In a search for structurally new inhibitors of fructose-1,6-bisphosphatase (F16BPase), substituted 2,3-dihydro-1H-cyclopenta[b]quinoline derivatives were synthesized. It has been shown that the 2,3-dihydro-1H-cyclopenta[b]quinoline moiety may represent a suitable scaffold for the synthesis of potent F16BPase inhibitors endowed with significantly lower EGFR tyrosine kinase inhibitory activity.
Rosini
Michela
M
Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Mancini
Francesca
F
Tarozzi
Andrea
A
Colizzi
Francesco
F
Andrisano
Vincenza
V
Bolognesi
Maria L
ML
Hrelia
Patrizia
P
Melchiorre
Carlo
C
D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D006597:Fructose-Bisphosphatase / Q000037:antagonists & inhibitors*; D006801:Humans; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000588:Amines; D004791:Enzyme Inhibitors; D011804:Quinolines; C037219:quinoline; D066246:ErbB Receptors; D006597:Fructose-Bisphosphatase