Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization

1991 ◽  
Vol 34 (8) ◽  
pp. 2579-2588 ◽  
Author(s):  
Mark Cushman ◽  
Dhanapalan Nagarathnam ◽  
D. Gopal ◽  
Asit K. Chakraborti ◽  
Chii M. Lin ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Tubulin Polymerization

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.

scholarly journals Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization

2021 ◽  
pp. 128131
Author(s):  
Shu-Yu Wang ◽  
Xu Liu ◽  
Ling-Wei Meng ◽  
Miao-Miao Li ◽  
Yin-Ru Li ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Tubulin Polymerization

scholarly journals Discovery of Novel 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization

2018 ◽  
Vol 9 (10) ◽  
pp. 974-979 ◽  
Author(s):  
Wenlong Li ◽  
Wen Shuai ◽  
Feijie Xu ◽  
Honghao Sun ◽  
Shengtao Xu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Tubulin Polymerization

scholarly journals Biological activity and interaction mechanism of the diketopiperazine derivatives as tubulin polymerization inhibitors

RSC Advances ◽  
2018 ◽  
Vol 8 (2) ◽  
pp. 1055-1064 ◽  
Author(s):  
Zhenhua Tian ◽  
Yanyan Chu ◽  
Hui Wang ◽  
Lili Zhong ◽  
Mengyan Deng ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Agents ◽  
Interaction Mechanism ◽  
Tubulin Polymerization ◽  
Tubulin Polymerization Inhibitors

Microtubules are a favorable target for development of anticancer agents.

Combretastatin A-4 inspired novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines as tubulin polymerization inhibitors, antimitotic and anticancer agents

MedChemComm ◽  
2014 ◽  
Vol 5 (6) ◽  
pp. 766-782 ◽  
Author(s):  
Nitesh Sanghai ◽  
Vaibhav Jain ◽  
Ranjan Preet ◽  
Somnath Kandekar ◽  
Sarita Das ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Tubulin Polymerization ◽  
Chromosomal Damage ◽  
Tubulin Polymerization Inhibitors

Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization inhibition, anticancer activity, anti-migration of cancer cells, chromosomal damage, and apoptosis have been developed.

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