Synthetis of Potential Anticancer Agents. XVI. S-Substituted Derivatives of 6-Mercaptopurine1a

1958 ◽  
Vol 80 (23) ◽  
pp. 6265-6271 ◽  
Author(s):  
Thomas P. Johnston ◽  
Lee B. Holum ◽  
John A. Montgomery
Keyword(s):  
Anticancer Agents ◽  
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.

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

New derivatives of imidazole as potential anticancer agents

Il Farmaco ◽  
1998 ◽  
Vol 53 (5) ◽  
pp. 342-345 ◽  
Author(s):  
Izabella Krȩżel
Keyword(s):  
Anticancer Agents ◽  
Derivatives Of

Design and Synthesis of Novel Urea Derivatives of Pyrimidine-Pyrazoles as Anticancer Agents

2021 ◽  
pp. 131937
Author(s):  
Purna Koteswara Rao Cherukumalli ◽  
Bhaskara Rao Tadiboina ◽  
Kali Charan Gulipalli ◽  
Srinu Bodige ◽  
Vishnu Nayak Badavath ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Urea Derivatives ◽  
Design And Synthesis ◽  
Derivatives Of

Amide derivatives of 4-azaindole: Design, synthesis, and EGFR targeting anticancer agents

2019 ◽  
Vol 50 (1) ◽  
pp. 71-84 ◽  
Author(s):  
Puli Venkat Swamy ◽  
Vukoti Kiran Kumar ◽  
Ruddarraju Radhakrishnam Raju ◽  
Regalla Venkata Reddy ◽  
Anindita Chatterjee ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Design Synthesis ◽  
Amide Derivatives ◽  
Derivatives Of

ChemInform Abstract: ERGOT ALKALOIDS. SYNTHESIS OF NITROSOUREA DERIVATIVES OF ERGOLINES AS POTENTIAL ANTICANCER AGENTS

1979 ◽  
Vol 10 (21) ◽  
Author(s):  
A. M. CRIDER ◽  
C. K. L. LU ◽  
H. G. FLOSS ◽  
J. M. CASSADY ◽  
J. A. CLEMENS
Keyword(s):  
Anticancer Agents ◽  
Ergot Alkaloids ◽  
Derivatives Of

scholarly journals Nanoprodrugs of NSAIDs Inhibit the Growth of U87-MG Glioma Cells

2010 ◽  
Vol 2010 ◽  
pp. 1-10 ◽  
Author(s):  
Bong-Seop Lee ◽  
Xiangpeng Yuan ◽  
Qijin Xu ◽  
Minhee K. Ko ◽  
Aruna K. Nalla ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Cell Growth ◽  
Anticancer Agents ◽  
Glioma Cells ◽  
Cell Counting ◽  
Malignant Cells ◽  
Spontaneous Emulsification ◽  
Superior Effect ◽  
Inflammatory Drugs ◽  
Derivatives Of

Several recent reports have demonstrated that nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit the growth of various malignant cells suggesting their application as anticancer agents. In this study, we prepared six nanometer-sized prodrugs (nanoprodrugs) of NSAIDs, ibuprofen, indomethacin, and naproxen through the spontaneous emulsification mechanism using monomeric and dimeric derivatives of the NSAIDs. We evaluated their effect on the proliferation of U87-MG glioma cells by cell counting, WST-1 cell proliferation reagent, and propidium iodide incorporation. The two ibuprofen nanoprodrugs inhibited the cell growth more potently than the indomethacin nanoprodrugs, whereas the naproxen nanoprodrugs did not show any significant effect. Remarkably, ibuprofen did not show any effect at an equimolar concentration. Approximately, 4.4% of the ibuprofen nanoprodrugs was found in the cell, whereas no ibuprofen could be detected suggesting that the superior effect of the nanoprodrugs can be attributed to the efficient cellular uptake of the nanoprodrugs.

scholarly journals A One-Pot Three-Component Synthesis and Investigation of the In Vitro Mechanistic Anticancer Activity of Highly Functionalized Spirooxindole-Pyrrolidine Heterocyclic Hybrids

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5581
Author(s):  
Raju Suresh Kumar ◽  
Dhaifallah M. Al-thamili ◽  
Abdulrahman I. Almansour ◽  
Natarajan Arumugam ◽  
Faruq Mohammad
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
One Pot ◽  
Major Pathway ◽  
Molecular Scaffold ◽  
Highly Active ◽  
Ft Ir ◽  
Derivatives Of ◽  
Unique Mechanism

With an aim to develop more effective and affordable anticancer agents possessing a unique mechanism of action, we designed and synthesized derivatives of spirooxindole-pyrrolidine heterocyclic hybrids in good yields through a one-pot three-component (3+2) cycloaddition strategy. The synthesized compounds were characterized thoroughly for the physicochemical properties by making use of FT-IR, NMR spectroscopy, and mass spectrometry. Further, these compounds have been evaluated for the influence of anticancer activity against HepG2 cells up to 200 µg/mL concentration. The highly active molecular scaffold was tested for the in-depth mechanistic studies, and it was found that the major pathway of cell death is apoptosis which occurs through the induction of reactive oxygen species followed by the involvement of caspases.

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