Design, synthesis and molecular modeling of new quinazolin-4(3H)-one based VEGFR-2 kinase inhibitors for potential anticancer evaluation

2021 ◽  
Vol 109 ◽  
pp. 104695
Author(s):  
Abdallah E. Abdallah ◽  
Sally I. Eissa ◽  
Maged Mohammed Saleh Al Ward ◽  
Reda R. Mabrouk ◽  
Ahmed B.M. Mehany ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Kinase Inhibitors ◽  
Design Synthesis

Design, synthesis and molecular modeling of biquinoline–pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors

2014 ◽  
Vol 24 (18) ◽  
pp. 4472-4476 ◽  
Author(s):  
Chetan B. Sangani ◽  
Jigar A. Makawana ◽  
Yong-Tao Duan ◽  
Yong Yin ◽  
Shashikant B. Teraiya ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Kinase Inhibitors ◽  
Design Synthesis ◽  
New Class ◽  
Her 2

Design, synthesis, molecular modeling, and ADMET studies of some pyrazoline derivatives as shikimate kinase inhibitors

2017 ◽  
Vol 27 (2) ◽  
pp. 546-559 ◽  
Author(s):  
Jainey P. James ◽  
K. Ishwar Bhat ◽  
Uttam A. More ◽  
Shrinivas D. Joshi
Keyword(s):  
Molecular Modeling ◽  
Kinase Inhibitors ◽  
Shikimate Kinase ◽  
Design Synthesis

Design, Synthesis, and Evaluation of Novel Imidazo[1,2-a][1,3,5]triazines and Their Derivatives as Focal Adhesion Kinase Inhibitors with Antitumor Activity

2014 ◽  
Vol 58 (1) ◽  
pp. 237-251 ◽  
Author(s):  
Pascal Dao ◽  
Nikaia Smith ◽  
Céline Tomkiewicz-Raulet ◽  
Expédite Yen-Pon ◽  
Marta Camacho-Artacho ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Focal Adhesion Kinase ◽  
Focal Adhesion ◽  
Kinase Inhibitors ◽  
Design Synthesis

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.

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