NAPHTHYL PHOSPHORAMIDATE DERIVATIVES OF BVdU AS POTENTIAL ANTICANCER AGENTS: DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION

2005 ◽  
Vol 24 (5-7) ◽  
pp. 485-489 ◽  
Author(s):  
C. Congiatu ◽  
C. McGuigan ◽  
W. G. Jiang ◽  
G. Davies ◽  
M. D. Mason
MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1812-1818 ◽  
Author(s):  
Junkai Huang ◽  
Zhuo Zhang ◽  
Peng Huang ◽  
Liqin He ◽  
Yong Ling

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.


2021 ◽  
Vol 31 ◽  
pp. 100608
Author(s):  
Indraganti Sreenivasa Murthy ◽  
Reddymasu Sireesha ◽  
Kolli Deepti ◽  
P. Srinivasa Rao ◽  
R. Ramesh Raju

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  

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.


2021 ◽  
Vol 6 (14) ◽  
pp. 3444-3452
Author(s):  
Asha V. Chate ◽  
Pramod A. Tagad ◽  
Giribala M. Bondle ◽  
Aniket P. Sarkate ◽  
Shailee V. Tiwari ◽  
...  

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 ◽  
...  

2019 ◽  
Vol 164 ◽  
pp. 562-575 ◽  
Author(s):  
Zhiqiang Yan ◽  
Shuyi Chong ◽  
Huiyun Lin ◽  
Qian Yang ◽  
Xin Wang ◽  
...  

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