scholarly journals Design, synthesis and biological evaluation of a series of new resveratrol analogues as potential anti-cancer agents

2019 ◽  
Vol 6 (9) ◽  
pp. 190125 ◽  
Author(s):  
Lifang Yang ◽  
Xuemei Qin ◽  
Hongcun Liu ◽  
Yanye Wei ◽  
Hailiang Zhu ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Docking Simulations ◽  
Human Cancer Cell Lines ◽  
Anti Cancer ◽  
Microscopy Analysis ◽  
Induced Apoptosis ◽  
Synthesis And Biological Evaluation

A series of novel resveratrol derivatives were designed, synthesized and evaluated as anti-cancer agents. Most of the compounds showed significant anti-proliferative activities against three human cancer cell lines (HepG2, A549 and Hela). Among these compounds, compound r displayed the most potent inhibitory activity and showed low cytotoxic activity. Cell apoptosis and cell cycle assays demonstrated that compound r significantly induced apoptosis ( p < 0.001) and arrested cell cycle at S phase. Immunofluorescence microscopy analysis showed compound r disrupted the tubulin network. Docking simulations supported the pharmacological results of compound r . It is believed that this work would be very useful for designing a new series of tubulin inhibitors.

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

scholarly journals Design, Synthesis, and Biological Evaluation of Aromatic Amide-Substituted Benzimidazole-Derived Chalcones. The Effect of Upregulating TP53 Protein Expression

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1162
Author(s):  
Lintao Wu ◽  
Yuting Yang ◽  
Zhijun Wang ◽  
Xi Wu ◽  
Feng Su ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Mechanistic Study ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Aromatic Amide ◽  
Synthesis And Biological Evaluation ◽  
Tp53 Protein

A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of compounds 3, 6, 9, 14, 15, 16 against HCT116 cells was significantly better than that that of 5-Fluorouracil (IC50: 94.63 µM). The antitumor activity of these compounds showed obvious differences between the wild type HCT116 and mutant HCT116 (TP53−/−) cells. A preliminary mechanistic study suggested that these compounds act by upregulating the expression of TP53 protein in tumor cells without inhibiting the MDM2-TP53 interaction.

scholarly journals Synthesis and Biological Evaluation of New Bis-Indolinone Derivatives Endowed with Cytotoxic Activity

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6277
Author(s):  
Rita Morigi ◽  
Elena Catanzaro ◽  
Alessandra Locatelli ◽  
Cinzia Calcabrini ◽  
Valentina Pellicioni ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Cell Cycle ◽  
Dna Damage ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Jurkat Cells ◽  
Human Cancer Cell ◽  
Antiproliferative Agents ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

A series of new Knoevenagel adducts, bearing two indolinone systems, has been synthesized and evaluated on 60 human cancer cell lines according to protocols available at the National Cancer Institute (Bethesda, MD, USA). Some derivatives proved to be potent antiproliferative agents, showing GI50 values in the submicromolar range. Compound 5b emerged as the most active and was further studied in Jurkat cells in order to determine the effects on cell-cycle phases and the kind of cell death induced. Finally, oxidative stress and DNA damage induced by compound 5b were also analyzed.

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 Synthesis and Biological Evaluation of Some 1,8-Naphthalimide-Acridinyl Hybrids

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Rui Chen ◽  
Caiying Yuan ◽  
Yogini Jaiswal ◽  
Lini Huo ◽  
Dianpeng Li ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Inhibition Activity ◽  
Dna Topoisomerase ◽  
Human Cancer Cell Lines ◽  
Pharmacological Mechanism ◽  
Electrophorus Electricus ◽  
Synthesis And Biological Evaluation ◽  
Mcf 7

In the present study, the synthesis of three 1,8-naphthalimide-acridinyl hybrids (2a, 2b, and 5b) using N-amido-1,8-naphthalimides (1 and 4) and acridinyl isothiocyanates is reported. The newly synthesized hybrids were evaluated for their anticancer activity in six human cancer cell lines (HL-60, MT-4, HepG2, HeLa, SK-OV-3, and MCF-7). Their inhibition activity against DNA-topoisomerase I (Topo I) and Electrophorus electricus acetylcholinesterase (AChE) was also studied. The results indicate that 2b displayed good cytotoxicity for MT-4, HepG2, HeLa, and SK-OV-3 with the IC50 values of 14.66 ± 0.31, 27.32 ± 2.67, 17.51 ± 0.34, and 32.26 ± 1.74 μM, respectively. All compounds, especially 2b, exhibited obvious bands corresponding to DNA fragments at 0.5 mM concentration, further confirming the pharmacological mechanism related to the Topo I inhibitory activities. In addition, compound 2a exhibited higher inhibition activity against AChE than 2b and 5b, with IC50 values of 0.32 ± 0.04 mM, and the acridinyl ring may contribute to the activity of 2a.

Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents

2012 ◽  
Vol 22 (23) ◽  
pp. 7268-7271 ◽  
Author(s):  
Tianwen Li ◽  
Yongchong Yang ◽  
Changmei Cheng ◽  
Amit K. Tiwari ◽  
Kamlesh Sodani ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of New (−)-Gossypol-Derived Schiff Bases and Hydrazones

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Vu Van Vu ◽  
Trinh Thi Nhung ◽  
Nguyen Thi Thanh ◽  
Luu Van Chinh ◽  
Vu Dinh Tien ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Schiff Bases ◽  
Cell Lines ◽  
Human Cancer ◽  
Structural Data ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
High Yields ◽  
Synthesis And Biological Evaluation

A series of 14 new (-)-gossypol Schiff bases and hydrazones have been synthesized via an in situ procedure in high yields. Structural data showed that all target compounds exist as the enamine tautomer. Bioassays showed that several compounds exhibited cytotoxic effects against three human cancer cell lines. Compound 8a showed the greatest cytotoxic effect against hepatocellular carcinoma (HepG2), lung carcinoma (LU-1), and breast cancer (MCF-7) cell lines with IC50 values of 20.93, 13.58, and 9.40 μM, respectively. However, in an antibacterial test, compounds 8a and 8b inhibited Staphylococcus aureus and Bacillus cereus and compound 8e inhibited only Staphylococcus aureus at the same MIC values of 1024 μg/ml.

scholarly journals Design, synthesis and biological evaluation of new carbazole derivatives as anti-cancer and anti-migratory agents

2018 ◽  
Vol 26 (4) ◽  
pp. 884-890 ◽  
Author(s):  
Cornelis P. Vlaar ◽  
Linette Castillo-Pichardo ◽  
Julia I. Medina ◽  
Cathyria M. Marrero-Serra ◽  
Ericka Vélez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Carbazole Derivatives ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of 1,3,4-Oxadiazole Fused Resveratrol Derivatives as Anticancer Agents

2020 ◽  
Vol 32 (8) ◽  
pp. 1967-1971
Author(s):  
Vema Venkata Naresh ◽  
Y. Bharathi Kumari ◽  
Mussulla Sridhar ◽  
Addada Ramakrishnam Raju ◽  
A. Srinivasa Rao
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Positive Control ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
Control Drug ◽  
Novel Target ◽  
Synthesis And Biological Evaluation ◽  
A549 Lung

A novel target compounds (9a-j) were design and synthesized and characterized by 1H & 13C NMR, ESI-MS spectral analysis. Further, these were tested for their anticancer activity against three human cancer cell lines such as MCF-7, MDA MB-231 (breast), A549 (Lung) and adriamycin was used as positive control. Among ten compounds, two compounds like 9b and 9j were showed a significant anticancer activity compared to control drug.

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