Design, synthesis, biological evaluation, and 3D-QSAR analysis of podophyllotoxin-dioxazole combination as tubulin targeting anticancer agents

2017 ◽  
Vol 90 (2) ◽  
pp. 236-243 ◽  
Author(s):  
Zi-Zhen Wang ◽  
Wen-Xue Sun ◽  
Xue Wang ◽  
Ya-Han Zhang ◽  
Han-Yue Qiu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
3D Qsar ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Qsar Analysis

scholarly journals Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells

RSC Advances ◽  
2020 ◽  
Vol 10 (43) ◽  
pp. 25517-25528
Author(s):  
Ahmad Junaid ◽  
Felicia Phei Lin Lim ◽  
Edward R. T. Tiekink ◽  
Anton V. Dolzhenko
Keyword(s):  
Breast Cancer ◽  
Triple Negative Breast Cancer ◽  
Anticancer Agents ◽  
Breast Cancer Cells ◽  
Triple Negative ◽  
3D Qsar ◽  
Qsar Model ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

New highly potent and selective 6,N2-diaryl-1,3,5-triazine-2,4-diamines were designed and prepared using the 3D-QSAR model developed earlier.

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.

Design, Synthesis and Biological Evaluation of Tetrahydrodibenzo[b,g][1,8]napthyridinones as Potential Anticancer Agents and Novel Aurora Kinases Inhibitors

2021 ◽  
Vol 6 (14) ◽  
pp. 3444-3452
Author(s):  
Asha V. Chate ◽  
Pramod A. Tagad ◽  
Giribala M. Bondle ◽  
Aniket P. Sarkate ◽  
Shailee V. Tiwari ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Aurora Kinases ◽  
Synthesis And Biological Evaluation

Design, Synthesis, and Biological Evaluation of (E)-Styrylbenzylsulfones as Novel Anticancer Agents

2008 ◽  
Vol 51 (1) ◽  
pp. 86-100 ◽  
Author(s):  
M. V. Ramana Reddy ◽  
Muralidhar R. Mallireddigari ◽  
Stephen C. Cosenza ◽  
Venkat R. Pallela ◽  
Nabisa M. Iqbal ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of tetrazole-containing RXRα ligands as anticancer agents

2019 ◽  
Vol 164 ◽  
pp. 562-575 ◽  
Author(s):  
Zhiqiang Yan ◽  
Shuyi Chong ◽  
Huiyun Lin ◽  
Qian Yang ◽  
Xin Wang ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates

2009 ◽  
Vol 17 (4) ◽  
pp. 1671-1680 ◽  
Author(s):  
Xiaochun Han ◽  
Chun Li ◽  
Michael D. Mosher ◽  
Kevin C. Rider ◽  
Peiwen Zhou ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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