Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors

2015 ◽  
Vol 23 (15) ◽  
pp. 4410-4422 ◽  
Author(s):  
Weike Liao ◽  
Gang Hu ◽  
Zhuang Guo ◽  
Deyu Sun ◽  
Lixia Zhang ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Quinoline Derivatives

scholarly journals New Quinoxaline Derivatives as Dual Pim-1/2 Kinase Inhibitors: Design, Synthesis and Biological Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 867
Author(s):  
Bruno Oyallon ◽  
Marie Brachet-Botineau ◽  
Cédric Logé ◽  
Thomas Robert ◽  
Stéphane Bach ◽  
...  
Keyword(s):  
Colorectal Carcinoma ◽  
Cancer Progression ◽  
Kinase Inhibitors ◽  
Integration Site ◽  
Leukemia Virus ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Proviral Integration Site ◽  
Quinoxaline Derivatives

Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression has been identified in a variety of hematologic (e.g., multiple myeloma or acute myeloid leukemia (AML)) and solid (e.g., colorectal carcinoma) tumors, playing a key role in cancer progression, metastasis, and drug resistance, and is linked to poor prognosis. These kinases are thus considered interesting targets in oncology. We report herein the design, synthesis, structure–activity relationships (SAR) and in vitro evaluations of new quinoxaline derivatives, acting as dual Pim1/2 inhibitors. Two lead compounds (5c and 5e) were then identified, as potent submicromolar Pim-1 and Pim-2 inhibitors. These molecules were also able to inhibit the growth of the two human cell lines, MV4-11 (AML) and HCT-116 (colorectal carcinoma), expressing high endogenous levels of Pim-1/2 kinases.

ChemInform Abstract: Synthesis and Preliminary Biological Evaluation of New Derivatives of the Marine Alkaloid Leucettamine B as Kinase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 41 (23) ◽  
pp. no-no
Author(s):  
Mansour Debdab ◽  
Steven Renault ◽  
Olivier Lozach ◽  
Laurent Meijer ◽  
Ludovic Paquin ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Marine Alkaloid ◽  
Derivatives Of

Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety

2019 ◽  
Vol 29 (1) ◽  
pp. 97-102 ◽  
Author(s):  
T.G. Shruthi ◽  
Sumesh Eswaran ◽  
Prasad Shivarudraiah ◽  
Shridhar Narayanan ◽  
Sangeetha Subramanian
Keyword(s):  
Biological Evaluation ◽  
Quinoline Derivatives
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