A New Series of 3-Alkyl Phosphate Derivatives of 4,5,6,7-Tetrahydro-1-d-ribityl-1H-pyrazolo[3,4-d]pyrimidinedione as Inhibitors of Lumazine Synthase:  Design, Synthesis, and Evaluation

2007 ◽  
Vol 72 (19) ◽  
pp. 7176-7184 ◽  
Author(s):  
Yanlei Zhang ◽  
Guangyi Jin ◽  
Boris Illarionov ◽  
Adelbert Bacher ◽  
Markus Fischer ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Lumazine Synthase ◽  
Alkyl Phosphate ◽  
Derivatives Of

Design, Synthesis, and Evaluation of 6-Carboxyalkyl and 6-Phosphonoxyalkyl Derivatives of 7-Oxo-8-ribitylaminolumazines as Inhibitors of Riboflavin Synthase and Lumazine Synthase

2002 ◽  
Vol 67 (16) ◽  
pp. 5807-5816 ◽  
Author(s):  
Mark Cushman ◽  
Donglai Yang ◽  
Stefan Gerhardt ◽  
Robert Huber ◽  
Markus Fischer ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Lumazine Synthase ◽  
Derivatives Of

Design, Synthesis and Evaluation of Novel Derivatives of Orotic Acid Amide as Potent Glucokinase Activators

2017 ◽  
Vol 14 (3) ◽  
pp. 252-261 ◽  
Author(s):  
Leilei Zhang ◽  
Shengquan Hu ◽  
Lei Lei ◽  
Yuliang Zhang ◽  
Lijing Zhang ◽  
...  
Keyword(s):  
Orotic Acid ◽  
Acid Amide ◽  
Design Synthesis ◽  
Glucokinase Activators ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

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