scholarly journals Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

MedChemComm ◽  
2017 ◽  
Vol 8 (6) ◽  
pp. 1158-1172 ◽  
Author(s):  
Yan-Cheng Yu ◽  
Wen-Bin Kuang ◽  
Ri-Zhen Huang ◽  
Yi-Lin Fang ◽  
Ye Zhang ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Hepg2 Cell ◽  
Antitumor Agents ◽  
Mitochondrial Pathway ◽  
Quinoline Derivatives ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
M Phase ◽  
Induced Apoptosis ◽  
Potential Antitumor

Novel 2-oxo-quinoline derivatives containing α-aminophosphonates were synthesized as antitumor agents. Compound 5b blocked HepG2 cell cycle at G2/M phase and induced apoptosis in mitochondrial pathway.

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 pharmacological evaluation of novel 4-phenoxyquinoline derivatives as potential antitumor agents

2015 ◽  
Vol 31 (5) ◽  
pp. 746-755 ◽  
Author(s):  
Hao Hu ◽  
Mingyan Jiang ◽  
Lijun Xie ◽  
Gang Hu ◽  
Cuirong Zhang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Potential Antitumor

scholarly journals Identification of Spiro-Fused Pyrrolo[3,4-a]pyrrolizines and Tryptanthrines as Potential Antitumor Agents: Synthesis and In Vitro Evaluation

2021 ◽  
Vol 22 (21) ◽  
pp. 11997
Author(s):  
Diana. K. Latypova ◽  
Stanislav V. Shmakov ◽  
Sofya A. Pechkovskaya ◽  
Alexander S. Filatov ◽  
Alexander V. Stepakov ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Hela Cells ◽  
Antitumor Agents ◽  
Hela Cell Lines ◽  
M Phase ◽  
Induced Apoptosis ◽  
Potential Antitumor

A series of heterocyclic compounds containing a spiro-fused pyrrolo[3,4-a]pyrrolizine and tryptanthrin framework have been synthesized and studied as potential antitumor agents. Cytotoxicity of products was screened against human erythroleukemia (K562) and human cervical carcinoma (HeLa) cell lines. Among the screened compounds. 4a, 4b and 5a were active against human erythroleukemia (K562) cell line, while 4a and 5a were active against cervical carcinoma (HeLa) cell line. In agreement with the DNA cytometry studies, the tested compounds have achieved significant cell-cycle perturbation with higher accumulation of cells in G2/M phase and induced apoptosis. Using confocal microscopy, we found that with 4a and 5a treatment of HeLa cells, actin filaments disappeared, and granular actin was distributed diffusely in the cytoplasm in 76–91% of cells. We discovered that HeLa cells after treatment with compounds 4a and 5a significantly reduced the number of cells with filopodium-like membrane protrusions (from 63 % in control cells to 29% after treatment) and a decrease in cell motility.

Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents

2014 ◽  
Vol 57 ◽  
pp. 30-42 ◽  
Author(s):  
Shunguang Zhou ◽  
Jianguo Ren ◽  
Mingmei Liu ◽  
Lixiang Ren ◽  
Yajing Liu ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Potential Antitumor

Synthesis, antiproliferative and apoptosis-inducing effects of novel asiatic acid derivatives containing α-aminophosphonates

RSC Advances ◽  
2016 ◽  
Vol 6 (67) ◽  
pp. 62890-62906 ◽  
Author(s):  
Ri-Zhen Huang ◽  
Cai-Yi Wang ◽  
Jian-Fei Li ◽  
Gui-Yang Yao ◽  
Ying-Ming Pan ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Antitumor Agents ◽  
Mitochondrial Pathway ◽  
S Phase ◽  
Asiatic Acid ◽  
Induced Apoptosis ◽  
Dependent Pathway

Novel asiatic acid derivatives containing α-aminophosphonates was designed and synthesized as antitumor agents. Compound 3d blocked the T24 cell cycle at G1/S phase by the p53-dependent pathway and induced apoptosis through mitochondrial pathway.

Design, Synthesis of Novel Quinazolone Alkaloids Derivatives as Potential Antitumor Agents

2011 ◽  
Vol 7 (4) ◽  
pp. 295-300
Author(s):  
Youguang Zheng ◽  
Min Sun ◽  
Yi Liu ◽  
Mingdong Li ◽  
Min Ji
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Potential Antitumor
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