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

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.

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.

Design and Synthesis of Indole Pyrimidine Scaffolds as Potential KSP Inhibitors and Anticancer Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 28-35
Author(s):  
Radhika Chelamalla ◽  
Ajitha Makula
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Agents ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Antimitotic Activity ◽  
Mcf 7

Background: Several biological activities like anticancer, anti-inflammatory, analgesic, antitubercular activities are reported for pyrimidine scaffolds. Extensive work on pyrimidine indole scaffolds is required for antimitotic activity. Objective: To synthesize a novel Indole Pyrimidine scaffold via an efficient synthetic method and to evaluate cytotoxic activity using various human cancer cell lines. Methods: 4,4-(3-substituted phenyl)-6-methyl-N-[(Z)-(5-methyl-2-oxo-indolin-3-ylidene)amino]-2- oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide derivatives were designed, synthesized and evaluated for cytotoxic activity. The structures were confirmed by IR, 1H NMR, C13NMR and Mass spectroscopy. The antiproliferative activities of the synthesized compounds were evaluated in vitro against human cancer cell lines including HeLa and MCF-7. Results: The results revealed that most of the compounds possessed moderate to excellent potency. Three among 10 molecules, showed more than 70% growth inhibition against all tested cancer cells. The nature of the substituent group (R) on the indole ring affected significantly the anti-proliferative activity of the molecules. The IC50 values of the most promising compound 4h are 76.4µM and 88.2µM against HeLa and MCF-7 respectively, which are closer to the standard compound doxorubicin. Conclusion: Molecular docking analysis demonstrated that 4b and 4d interact and bind efficiently with KSP binding site. The preliminary results made us investigate for further development of potent indole-pyrimidine scaffolds as cytotoxic agents

In vitro biological evaluation of novel 7-O-dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines

2008 ◽  
Vol 18 (20) ◽  
pp. 5431-5434 ◽  
Author(s):  
Marco Bonesi ◽  
Rosa Tundis ◽  
Brigitte Deguin ◽  
Monica R. Loizzo ◽  
Federica Menichini ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines
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