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.

scholarly journals Comprehensive Evaluation of Biological Effects of Pentathiepins on Various Human Cancer Cell Lines and Insights into Their Mode of Action

2021 ◽  
Vol 22 (14) ◽  
pp. 7631
Author(s):  
Lisa Wolff ◽  
Siva Sankar Murthy Bandaru ◽  
Elias Eger ◽  
Hoai-Nhi Lam ◽  
Martin Napierkowski ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Strand Breaks ◽  
Human Cancer Cell Lines

Pentathiepins are polysulfur-containing compounds that exert antiproliferative and cytotoxic activity in cancer cells, induce oxidative stress and apoptosis, and inhibit glutathione peroxidase (GPx1). This renders them promising candidates for anticancer drug development. However, the biological effects and how they intertwine have not yet been systematically assessed in diverse cancer cell lines. In this study, six novel pentathiepins were synthesized to suit particular requirements such as fluorescent properties or improved water solubility. Structural elucidation by X-ray crystallography was successful for three derivatives. All six underwent extensive biological evaluation in 14 human cancer cell lines. These studies included investigating the inhibition of GPx1 and cell proliferation, cytotoxicity, and the induction of ROS and DNA strand breaks. Furthermore, selected hallmarks of apoptosis and the impact on cell cycle progression were studied. All six pentathiepins exerted high cytotoxic and antiproliferative activity, while five also strongly inhibited GPx1. There is a clear connection between the potential to provoke oxidative stress and damage to DNA in the form of single- and double-strand breaks. Additionally, these studies support apoptosis but not ferroptosis as the mechanism of cell death in some of the cell lines. As the various pentathiepins give rise to different biological responses, modulation of the biological effects depends on the distinct chemical structures fused to the sulfur ring. This may allow for an optimization of the anticancer activity of pentathiepins in the future.

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.

Synthesis and biological evaluation of sapinofuranones A,B and 1,2,3-triazole-sapinofuranone hybrids as cytotoxic agents

RSC Advances ◽  
2016 ◽  
Vol 6 (103) ◽  
pp. 101501-101512 ◽  
Author(s):  
K. Siva Nagi Reddy ◽  
Gowravaram Sabitha ◽  
Y. Poornachandra ◽  
C. Ganesh Kumar
Keyword(s):  
Total Synthesis ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

The total synthesis of sapinofuranones A,B and ent-sapinofuranones A,B and L-factor and a series of novel 1,2,3-triazole-sapinofuranone hybrids is described and their cytotoxicity against four human cancer cell lines (A549, MDA-MB-231, DU145 and HepG2) was evaluated.

scholarly journals Synthesis and Biological Evaluation of Lipophilic 1,4-Naphthoquinone Derivatives against Human Cancer Cell Lines

Molecules ◽  
2015 ◽  
Vol 20 (7) ◽  
pp. 11994-12015 ◽  
Author(s):  
Shao-Hung Wang ◽  
Chih-Yu Lo ◽  
Zhong-Heng Gwo ◽  
Hong-Jhih Lin ◽  
Lih-Geeng Chen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d]imidazoles and imidazo[4,5-f][1,10]phenanthrolines

2016 ◽  
Vol 14 (16) ◽  
pp. 3889-3905 ◽  
Author(s):  
Alpa Patel ◽  
Swee Y. Sharp ◽  
Katelan Hall ◽  
William Lewis ◽  
Malcolm F. G. Stevens ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Cell Lines ◽  
Heat Shock Protein 70 ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Induction Of Apoptosis ◽  
Synthesis And Biological Evaluation

Fused imidazoles inhibit growth of human cancer cell lines, and the Hsp70 pathway in cells, and induce apoptosis.

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.

N-Deacetyl-N-aminoacylthiocolchicine Derivatives:  Synthesis and Biological Evaluation on MDR-Positive and MDR-Negative Human Cancer Cell Lines

1999 ◽  
Vol 42 (25) ◽  
pp. 5272-5276 ◽  
Author(s):  
Maria Luisa Gelmi ◽  
Sabrina Mottadelli ◽  
Donato Pocar ◽  
Antonella Riva ◽  
Ezio Bombardelli ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of 3-(3,4,5-Trimethoxyphenyl)- 5-(2-(5-arylbenzo[b]thiophen-3-yl)oxazol-5-yl)isoxazole Derivatives as Anticancer Agents

2020 ◽  
Vol 17 (5) ◽  
pp. 345-351
Author(s):  
Syndla Premalatha ◽  
G. Rambabu ◽  
Islavathu Hatti ◽  
Dittakavi Ramachandran
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Isoxazole Derivatives

A new series of 3-(3,4,5-trimethoxyphenyl)-5-(2-(5-arylbenzo[b]thiophen-3-yl)oxa zol-5- yl)isoxazole derivatives were designed and synthesized. All these derivatives were evaluated for their anticancer activity against various human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer)-four human cancer cell lines by using MTT assay. Here, etoposide was used as a standard reference drug and most of the compounds were exhibited good anticancer activity with respect to cell lines. Among all compounds, five compounds 11b, 11c, 11f, 11i and 11j showed more potent activity than standard drug, in which, compound 11f was the most promising compound.

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