Design, synthesis, and biological evaluation of substituted 2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamine related compounds as fructose-1,6-bisphosphatase inhibitors
作者:Michela Rosini、Francesca Mancini、Andrea Tarozzi、Francesco Colizzi、Vincenza Andrisano、Maria L. Bolognesi、Patrizia Hrelia、Carlo Melchiorre
DOI:10.1016/j.bmc.2006.07.059
日期:2006.12
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.
为了寻找结构上新的果糖-1,6-双磷酸酶(F16BPase)抑制剂,合成了取代的2,3-二氢-1H-环戊[b]喹啉衍生物。已经显示出2,3-二氢-1H-环戊基[b]喹啉部分可以代表用于合成具有显着较低的EGFR酪氨酸激酶抑制活性的有效F16BPase抑制剂的支架。