scholarly journals Cytotoxic and Antitumor Activity of some Coumarin Derivatives

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Hugo A. Garro ◽  
Guillermo F. Reta ◽  
Osvaldo J. Donadel ◽  
Carlos R. Pungitore
Keyword(s):  
Antitumor Activity ◽  
Tumor Cell ◽  
Cell Lines ◽  
Dna Polymerase ◽  
Antitumor Drugs ◽  
Tumor Cell Lines ◽  
Coumarin Derivatives ◽  
Lead Compound ◽  
Taq Dna Polymerase ◽  
Human Solid Tumor

Several natural and synthetic coumarins were assayed against different cancer cell lines. Four of them have shown cytotoxicity against a panel of three human solid tumor cell lines (HeLa, T-47D, and WiDr) and a clearly activity/hydrophobicity relationship. Compound 13 proved to be the most active product in all cell lines tested, with values of 8.0 (±0.38) μM against HeLa cells and also able to inhibit Taq DNA polymerase. This dual activity of 13 makes it a candidate to be considered as a “lead” compound in the search for novel antitumor drugs.

Antiproliferative activity of novel benzo[b][1,6]naphthyridines in human solid tumor cell lines

2010 ◽  
Vol 20 (5) ◽  
pp. 1504-1506 ◽  
Author(s):  
Simonas Rudys ◽  
Carla Ríos-Luci ◽  
Eduardo Pérez-Roth ◽  
Inga Cikotiene ◽  
José M. Padrón
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Solid Tumor ◽  
Antiproliferative Activity ◽  
Tumor Cell Lines ◽  
Human Solid Tumor

scholarly journals Lipophilic Salirasib analogs with enhanced antiproliferative activity against human solid tumor cell lines

2021 ◽  
Author(s):  
Exequiel O. J. Porta ◽  
María Sol Ballari ◽  
José M. Padrón ◽  
Guillermo R. Labadie
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Cancer Cell ◽  
Solid Tumor ◽  
Antiproliferative Activity ◽  
In Silico ◽  
Tumor Cell Lines ◽  
Human Solid Tumor ◽  
Physicochemical Features ◽  
Sar Analysis

Aim: We proposed to determine the antiproliferative activity of a series of synthetic salirasib analogs, presenting or not a 1,2,3-triazole linker, against five different cancer cell lines. Results: Bioassay, cheminformatic, and in silico ADME-Tox allowed the identification of new potent analogs. SAR analysis allowed the identification of structural and physicochemical features that benefit the antiproliferative activity. Conclusion: Isoprenyl R chains with three or more isoprene units, or long aliphatic R chains are the preferred ones within the active compounds. Likewise, we have identified three compounds with better activity profiles than salirasib against all the cell lines tested.

scholarly journals Glutamine as a Regulator of DNA and Protein Biosynthesis in Human Solid Tumor Cell Lines

1996 ◽  
Vol 224 (2) ◽  
pp. 189-197 ◽  
Author(s):  
Masafumi Wasa ◽  
Barrie P. Bode ◽  
Steven F. Abcouwer ◽  
Cynthia L. Collins ◽  
Kenneth K. Tanabe ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Solid Tumor ◽  
Protein Biosynthesis ◽  
Tumor Cell Lines ◽  
Human Solid Tumor

scholarly journals Antitumor Activity In Vitro Provided by N-Alkyl-Nitroimidazole Compounds

2020 ◽  
Vol 14 (1) ◽  
pp. 45-48
Author(s):  
Janny A. Villa-Pulgarin ◽  
Constain H. Salamanca ◽  
Jose Oñate-Garzón ◽  
Ruben E Varela-M
Keyword(s):  
Antitumor Activity ◽  
Tumor Cell ◽  
Cell Lines ◽  
Alkyl Chain ◽  
Imidazole Ring ◽  
Antitumoral Activity ◽  
Lung Cells ◽  
Tumor Cell Lines ◽  
A549 Lung

Background: Cancer is one of the most common diseases in the world, with over 18 million new cases estimated in 2018. Many of the drugs used for cancer can have significant adverse effects and variable effectiveness. Nitroimidazoles are prodrugs that usually have shown antimicrobial activity specifically antiparasitic. However, its antitumor activity in vitro has barely been explored. Objective: The aim of this study is to determine the influence of the length of the substituted N-alkyl chain in the imidazole ring on the antitumor activity in vitro. Methods: Four nitroimidazoles were obtained by chemical synthesis varying the length of the substituted N-alkyl chain from methyl to butyl. The antitumor activity of N-alkyl-nitroimidazoles was evaluated by MTT assay employing two tumor cell lines (MDA-MB231 and A549). Results: In this study, it was reported that N-alkyl nitroimidazoles exhibited an LC50 as low as 16.7 µM in breast tumor cells MDA-MB231 while in normal Vero kidney cells, the LC50 was around 30 µM. It was also reported that the length of the substituted N-Alkyl chain in the imidazole ring affects the antitumoral activity in A549 lung cells. Conclusion: Increasing the length of the substituted N-Alkyl chain in the imidazole ring decreased the antitumor activity against only A549 cancer cells. N-alkyl nitroimidazoles exhibited considerable selectivity towards tumor cell lines.

scholarly journals Cytotoxic Bioactivity of Some Phenylpropanoic Acid Derivatives

2012 ◽  
Vol 7 (10) ◽  
pp. 1934578X1200701 ◽  
Author(s):  
Guillermo F. Reta ◽  
Carlos E. Tonn ◽  
Carla Ríos-Luci ◽  
Leticia G. León ◽  
Eduardo Pérez-Roth ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Solid Tumor ◽  
Tumor Cell Lines ◽  
Molecular Scaffold ◽  
Human Solid Tumor ◽  
Antiproliferative Activities

In this study, we synthesized a series of phenylpropanoic acid derivatives based on modifications at four selected points of the molecular scaffold. The in vitro antiproliferative activities of the compounds were examined in representative human solid tumor cell lines. A SAR was established pointing out the relevance of the substituents. The best activity profiles were obtained for the derivatives bearing more lipophilic esters (GI50 3.1-21 μM).

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