scholarly journals Design Synthesis and Biological Evaluation of Dithiocarbamate Substituted 2-Aminobenzothiazole Derivatives as Proviral Integration Site of Moloney Murine Leukaemia Virus 1 Kinase Inhibitors

2020 ◽  
Vol 82 (6) ◽  
Author(s):  
P. SAI HARSHITA ◽  
CH. SUPRIYA ◽  
SELINA SRAVANTHI ◽  
V. JYOTHI ◽  
S. R. PEDDI ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Integration Site ◽  
Biological Evaluation ◽  
Proviral Integration ◽  
Design Synthesis ◽  
Leukaemia Virus ◽  
Murine Leukaemia Virus ◽  
Proviral Integration Site ◽  
Synthesis And Biological Evaluation ◽  
Moloney Murine Leukaemia Virus

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.

Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation

2020 ◽  
Vol 30 (16) ◽  
pp. 127327
Author(s):  
Zhicheng Su ◽  
Tingyuan Yang ◽  
Jie Wang ◽  
Mengzhen Lai ◽  
Linjiang Tong ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Egfr Kinase

scholarly journals Design, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors

2011 ◽  
Vol 54 (20) ◽  
pp. 7427-7431 ◽  
Author(s):  
Christine Dyrager ◽  
Linda Nilsson Möllers ◽  
Linda Karlsson Kjäll ◽  
John Patrick Alao ◽  
Peter Dinér ◽  
...  
Keyword(s):  
Map Kinase ◽  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
P38 Map Kinase ◽  
Design Synthesis ◽  
P38 Map Kinase Inhibitors ◽  
Synthesis And Biological Evaluation
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