Synthesis and biological activities of pyrazolo[3,4- g]quinoxaline derivatives

The synthesis of new pyrazolo[3,4- g]quinoxaline derivatives, as well as their Pim kinases (Pim-1, Pim-2, Pim-3) inhibitory potencies and in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PA1, PC3 and DU145) are described. The re...

Full description

Saved in:
Bibliographic Details
Published in:European journal of medicinal chemistry 2010-11, Vol.45 (11), p.5520-5526
Main Authors: Gavara, Laurent, Saugues, Emmanuelle, Alves, Georges, Debiton, Eric, Anizon, Fabrice, Moreau, Pascale
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
General aspects
Humans
In vitro antiproliferative activities
Kinase inhibition
Magnetic Resonance Spectroscopy
Medical sciences
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Pyrazolo[3,4- g]quinoxaline
Quinoxalines - chemical synthesis
Quinoxalines - pharmacology
Spectrometry, Mass, Electrospray Ionization
Spectrophotometry, Infrared
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The synthesis of new pyrazolo[3,4- g]quinoxaline derivatives, as well as their Pim kinases (Pim-1, Pim-2, Pim-3) inhibitory potencies and in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PA1, PC3 and DU145) are described. The results obtained in this preliminary structure–activity relationship study have pointed out that most of the compounds in this series exhibited interesting in vitro Pim-3 kinase inhibitory potencies. Moreover, some of the tested compounds have demonstrated favorable antiproliferative potencies. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2010.08.067