scholarly journals Naphthalene substituted benzo[c]coumarins: Synthesis, characterization and evaluation of antibacterial activity and cytotoxicity

2019 ◽  
Vol 25 (1) ◽  
pp. 146-151
Author(s):  
Mrugesh Patel ◽  
Kaushal Patel
Keyword(s):  
Antibacterial Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Spectroscopic Techniques ◽  
Cell Viability Assay ◽  
Human Cancer Cell Lines ◽  
Significant Growth ◽  
Growth Inhibitory

AbstractNovel congeners of naphthalene substituted benzo[c]coumarins (2a-f) were synthesized by reaction of various 3-coumarinoyl methyl pyridinium bromide salts (1a-d) with a selected set of acetyl naphthalene in the presence of sodium acetate in refluxing glacial acetic acid. Structures of the synthesized compounds were confirmed by elemental analysis and by various spectroscopic techniques such as 1H-NMR, 13C-NMR, DEPT, and MS spectral data. Synthesised compounds were screened for antibacterial activity and cytotoxicity against different human cancer cell lines including cervix cancer (HeLa), breast cancer (MCF-7) and lung cancer (A549) using tetrazolium dye 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell viability assay. Although with varying degrees, a significant growth inhibitory and cytotoxic effects were observed on all three cancer cell lines. Compounds 2b and 2e showed significant growth inhibitory and cytotoxicity against aforementioned cancer cell lines.

Synthesis of C4-fluorinated solamins and their growth inhibitory activity against human cancer cell lines

2008 ◽  
Vol 18 (24) ◽  
pp. 6451-6453 ◽  
Author(s):  
Naoto Kojima ◽  
Hiromi Hayashi ◽  
Satoshi Suzuki ◽  
Hiroaki Tominaga ◽  
Naoyoshi Maezaki ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

ChemInform Abstract: Design and Synthesis of C35-Fluorinated Solamins and Their Growth Inhibitory Activities Against Human Cancer Cell Lines.

ChemInform ◽  
2012 ◽  
Vol 43 (9) ◽  
pp. no-no
Author(s):  
Naoto Kojima ◽  
Yuki Suga ◽  
Hiromi Hayashi ◽  
Takao Yamori ◽  
Takehiko Yoshimitsu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Growth Inhibitory ◽  
Inhibitory Activities

No Correlation between GSH Levels in Human Cancer Cell Lines and the Cell Growth Inhibitory Activities of Platinum Diamine Complexes

2004 ◽  
Vol 337 (12) ◽  
pp. 668-671 ◽  
Author(s):  
Boubakari ◽  
Karin Bracht ◽  
Christian Neumann ◽  
Renate Grünert ◽  
Patrick J. Bednarski
Keyword(s):  
Cell Growth ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Growth Inhibitory ◽  
Inhibitory Activities

scholarly journals Modulating the activity of short arginine-tryptophan containing antibacterial peptides with N-terminal metallocenoyl groups

2012 ◽  
Vol 8 ◽  
pp. 1753-1764 ◽  
Author(s):  
H Bauke Albada ◽  
Alina-Iulia Chiriac ◽  
Michaela Wenzel ◽  
Maya Penkova ◽  
Julia E Bandow ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Growth Inhibition ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Inhibition Studies ◽  
Kinetics Of

A series of small synthetic arginine and tryptophan containing peptides was prepared and analyzed for their antibacterial activity. The effect of N-terminal substitution with metallocenoyl groups such as ferrocene (FcCO) and ruthenocene (RcCO) was investigated. Antibacterial activity in different media, growth inhibition, and killing kinetics of the most active peptides were determined. The toxicity of selected derivatives was determined against erythrocytes and three human cancer cell lines. It was shown that the replacement of an N-terminal arginine residue with a metallocenoyl moiety modulates the activity of WRWRW-peptides against Gram-positive and Gram-negative bacteria. MIC values of 2–6 µM for RcCO-W(RW)2 and 1–11 µM for (RW)3 were determined. Interestingly, W(RW)2-peptides derivatized with ferrocene were significantly less active than those derivatized with ruthenocene which have similar structural but different electronic properties, suggesting a major influence of the latter. The high activities observed for the RcCO-W(RW)2- and (RW)3-peptides led to an investigation of the origin of activity of these peptides using several important activity-related parameters. Firstly, killing kinetics of the RcCO-W(RW)2-peptide versus killing kinetics of the (RW)3 derivative showed faster reduction of the colony forming units for the RcCO-W(RW)2-peptide, although MIC values indicated higher activity for the (RW)3-peptide. This was confirmed by growth inhibition studies. Secondly, hemolysis studies revealed that both peptides did not lead to significant destruction of erythrocytes, even up to 500 µg/mL for (RW)3 and 250 µg/mL for RcCO-W(RW)2. In addition, toxicity against three human cancer cell lines (HepG2, HT29, MCF7) showed that the (RW)3-peptide had an IC50 value of ~140 µM and the RcW(RW)2 one of ~90 µM, indicating a potentially interesting therapeutic window. Both the killing kinetics and growth inhibition studies presented in this work point to a membrane-based mode of action for these two peptides, each having different kinetic parameters.

scholarly journals Design, Synthesis and Structural Confirmation of a Series of 2-(Thiophen-2-yl)- 4H-chromen-3-yl-sulfonate Derivatives and Preliminary Investigation of Their Antioxidant and Anticancer Potentials

2021 ◽  
Author(s):  
Jialin Zang ◽  
Ming Bu ◽  
Jifang Yang ◽  
Lu Han ◽  
Zhen Lv
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A series of novel 2-(thiophen-2-yl)-4H-chromen-3-yl-sulfonate derivatives (4a-4n) were synthesized and investigated for their in vitro free radical scavenging potential as well as cytotoxic efficacies against selected cancer cell lines. The cytotoxicity of the 4H-chromene derivatives (4a‑4n) was evaluated according to three human cancer cell lines (HepG2, A549, HeLa) by utilizing a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Accordingly, part of the results exhibited better cytotoxic activities than that of the positive controls (4H-chromen-4-one and apigenin). Among them, compounds 4c-4g exhibited better training to the positive control against the three human cancer cell lines (half maximal inhibitory concentration (IC50) = 3.87 ± 0.12 to 21.38 ± 0.52 μM). Moreover, the extract of the 4H-chromene derivatives (4a‑4n) showed better activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis-3‑ethylbenzothiazoline-6-sulfonic acid (ABTS) in antioxidant assays compared to that of the positive control ascorbic acid (IC50 = 12.72 ± 0.27, 5.09 ± 0.21 μg mL-1). Thus, it can be confirmed from the bioassay results that the overall structural design, as well as proper substitution, is crucial in delivering anticipated biological effects. In this regard, spectroscopic techniques such as 1H nuclear magnetic resonance (NMR), 13C NMR, and high-resolution mass spectrometry (HRMS) were also carried out to confirm the final structures.

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