Design, Synthesis and Antimalarial Activity of Some New Aminoalcoholpyrrolo[1,2-a]quinoxaline Derivatives

2016 ◽  
Vol 13 (9) ◽  
pp. 932-942 ◽  
Author(s):  
Jean Guillon ◽  
Stéphane Moreau ◽  
Luisa Ronga ◽  
Louise Basmacyian ◽  
Anita Cohen ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis ◽  
Quinoxaline 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.

scholarly journals Synthetic spirocyclic endoperoxides: new antimalarial scaffolds

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 357-362 ◽  
Author(s):  
Margherita Brindisi ◽  
Sandra Gemma ◽  
Sanil Kunjir ◽  
Luisa Di Cerbo ◽  
Simone Brogi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antimalarial Activity ◽  
Design Synthesis ◽  
Docking Calculation

Design, synthesis and molecular docking calculation studies led to the identification of novel spirocyclic peroxides with in vitro and in vivo antimalarial activity.

scholarly journals Design, Synthesis and Antimalarial Activity of Novel, Quinoline-Based, Zinc Metallo-Aminopeptidase Inhibitors.

ChemInform ◽  
2003 ◽  
Vol 34 (50) ◽  
Author(s):  
Marian Flipo ◽  
Isabelle Florent ◽  
Philippe Grellier ◽  
Christian Sergheraert ◽  
Rebecca Deprez-Poulain
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis ◽  
Aminopeptidase Inhibitors

Design, synthesis and in vitro antimalarial activity of spiroperoxides

Tetrahedron ◽  
2006 ◽  
Vol 62 (33) ◽  
pp. 7699-7711 ◽  
Author(s):  
Hong-Xia Jin ◽  
Qi Zhang ◽  
Hye-Sook Kim ◽  
Yusuke Wataya ◽  
He-Hua Liu ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis

ChemInform Abstract: The Design, Synthesis and Biological Evaluation of Stable Ozonides with Antimalarial Activity.

ChemInform ◽  
2010 ◽  
Vol 27 (36) ◽  
pp. no-no
Author(s):  
L.-C. DE ALMEIDA BARBOSA ◽  
D. CUTLER ◽  
J. MANN ◽  
M. J. CRABBE ◽  
G. C. KIRBY ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: Synthesis, and in vitro antimalarial activity

2008 ◽  
Vol 16 (20) ◽  
pp. 9133-9144 ◽  
Author(s):  
Jean Guillon ◽  
Stéphane Moreau ◽  
Elisabeth Mouray ◽  
Véronique Sinou ◽  
Isabelle Forfar ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Quinoxaline Derivatives

The design, synthesis and biological evaluation of stable ozonides with antimalarial activity

1996 ◽  
pp. 1101 ◽  
Author(s):  
Luiz-Claudio de Almeida Barbosa ◽  
David Cutler ◽  
John Mann ◽  
M. James Crabbe ◽  
Geoffrey C. Kirby ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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