scholarly journals Proteinaceous Secretory Metabolites of Probiotic Human Commensal Enterococcus hirae 20c, E. faecium 12a and L12b as Antiproliferative Agents Against Cancer Cell Lines

2018 ◽  
Vol 9 ◽  
Author(s):  
Preeti Sharma ◽  
Sumanpreet Kaur ◽  
Raminderjit Kaur ◽  
Manpreet Kaur ◽  
Sukhraj Kaur
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Enterococcus Hirae ◽  
Antiproliferative Agents

scholarly journals Design, Synthesis and Biological Evaluation of a New Series of 1-Aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea Derivatives as Antiproliferative Agents

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2108 ◽  
Author(s):  
Chuanming Zhang ◽  
Xiaoyu Tan ◽  
Jian Feng ◽  
Ning Ding ◽  
Yongpeng Li ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
A549 Cells ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Urea Derivatives ◽  
Antiproliferative Agents

To discover new antiproliferative agents with high efficacy and selectivity, a new series of 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea derivatives (7a–7t) were designed, synthesized and evaluated for their antiproliferative activity against A549, HCT-116 and PC-3 cancer cell lines in vitro. Most of the target compounds demonstrated significant antiproliferative effects on all the selective cancer cell lines. Among them, the target compound, 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-{4-{{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methyl}thio}phenyl}urea (7i) was identified to be the most active one against three cell lines, which was more potent than the positive control with an IC50 value of 1.53 ± 0.46, 1.11 ± 0.34 and 1.98 ± 1.27 μM, respectively. Further cellular mechanism studies confirmed that compound 7i could induce the apoptosis of A549 cells in a concentration-dependent manner and elucidated compound 7i arrests cell cycle at G1 phase by flow cytometry analysis. Herein, the studies suggested that the 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea skeleton might be regarded as new chemotypes for designing effective antiproliferative agents.

scholarly journals Synthesis and Antiproliferative activity in vitro of Amidino Substituted 2-phenylbenzazoles

2019 ◽  
Vol 92 (2) ◽  
pp. 181-189 ◽  
Author(s):  
Livio Racané ◽  
Kristina Butković ◽  
Irena Martin-Kleiner ◽  
Marijeta Kralj ◽  
Grace Karminski-Zamola ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Benzimidazole Derivatives ◽  
Antiproliferative Agents ◽  
Benzothiazole Derivatives

Within this work we describe the synthesis of versatile substituted 2-phenyl benzothiazole 3–10 and 2-phenylbenzimidazole 12–19 derivatives bearing amidino groups. Furthermore, the synthesized compounds were explored for their antiproliferative activity in vitro on three cancer cell lines. Tested compounds showed moderate to strong antiproliferative activity. Furthermore, the type of the attached amidino group on benzazole nuclei has the significant impact on the antiproliferative activity only within benzimidazole derivatives with 2-imidazolinyl substituted derivatives being more active in comparison to amidino substituted analogues. All obtained results revealed that this type of benzothiazole derivatives have a great potential for further optimization and development of more efficient potential antiproliferative agents.

scholarly journals In vitro antiproliferative activity of some fluoro-substituted benzimidazole-based scaffolds

2021 ◽  
Vol 4 (1) ◽  
pp. 10-17
Author(s):  
Ronak Haj Ersan ◽  
Nizami Duran
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Positive Control ◽  
Human Cells ◽  
Benzimidazole Derivatives ◽  
Antiproliferative Agents

In the present work, a series of fluoro-substituted benzimidazole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of these compounds was investigated using MTT assay. Fluoro-substituted benzimidazole derivatives showed significant antiproliferative activity against all the tested cancer cell lines. All the derivatives were found to be less toxic as compared to methotrexate (positive control) in human cells, indicating selective and efficient antiproliferative activity of these benzimidazole derivatives. These findings suggest that compounds ORT14 and ORT15 among this series are most effective and have potential for detailed investigations.

scholarly journals Synthesis of MeON-Glycoside Derivatives of Oleanolic Acid by Neoglycosylation and Evaluation of Their Cytotoxicity against Selected Cancer Cell Lines

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 772
Author(s):  
Zhichao Du ◽  
Guolong Li ◽  
Xiaoyang Zhou ◽  
Jian Zhang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Oleanolic Acid ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Cell Counting ◽  
Antiproliferative Agents ◽  
Antiproliferative Activities

A series of C-3 and C-28 MeON-neoglycosides of oleanolic acid were designed and synthesized by neoglycosylation as potential antiproliferative agents. Their cytotoxicity was evaluated in vitro against five human cancer cell lines: human non-small cell lung cancer cell line (A549), human melanoma cell line (A375), human colon cancer cell line (HCT116), human liver carcinoma cell line (HepG2), human breast adenocarcinoma cell line (MCF-7) by the Cell Counting Kit-8 (CCK-8) assay. Most of C-3 and C-28 MeON-neoglycosides of oleanolic acid exhibited notably inhibitory effects against the tested cancer cells and more sensitive to HepG2 cells than 5-Fluorouracil (5-FU). Structure-activities relationship (SAR) analysis revealed that sugar types and the d/l configuration of sugars would significantly affect their antiproliferative activities of neoglycosides. Among them, compound 8a (28-N-methoxyaminooleanane-β-d-glucoside) exhibited the most potent antiproliferative activities against HepG2 cells with IC50 values of 2.1 µM. Further pharmacological experiments revealed that compound 8a could cause morphological changes and cell cycle arrest at G0/G1 phase and induce apoptosis in HepG2 cells. These results suggested that neoglycosylation could provide a rapid strategy for the discovery of potential antiproliferative agents and their possible pharmacological mechanisms need more further research.

Novel phosphine sulphide gold(i) complexes: topoisomerase I inhibitors and antiproliferative agents

2020 ◽  
Vol 49 (23) ◽  
pp. 7852-7861
Author(s):  
Endika Martín-Encinas ◽  
Verónica Conejo-Rodríguez ◽  
Jesús A. Miguel ◽  
Jesús M. Martínez-Ilarduya ◽  
Gloria Rubiales ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Topoisomerase I ◽  
Cancer Cell Lines ◽  
Antiproliferative Agents ◽  
Topoisomerase I Inhibitors ◽  
Phosphine Sulfide

Gold(i) increases the cytotoxicity of phosphine sulfide quinolines against cancer cell lines, while heterocycles maintain the TopI inhibitory activity.

797: Noggin Blocks the Osteoinductive Properties of Human Prostate Cancer Cell Lines

2006 ◽  
Vol 175 (4S) ◽  
pp. 258-258
Author(s):  
Ruth Schwaninger ◽  
Cyrill A. Rentsch ◽  
Antoinette Wetterwald ◽  
Irena Klima ◽  
Gabri Van der Pluijm ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Human Prostate ◽  
Human Prostate Cancer ◽  
Human Prostate Cancer Cell ◽  
Prostate Cancer Cell Lines
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