scholarly journals Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 1956 ◽  
Author(s):  
Leydi Moreno ◽  
Jairo Quiroga ◽  
Rodrigo Abonia ◽  
Jonathan Ramírez-Prada ◽  
Braulio Insuasty
Keyword(s):  
Anticancer Agents ◽  
Human Tumor ◽  
Aromatic Aldehydes ◽  
High Yield ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Microwave Assisted ◽  
The Us ◽  
Cyclocondensation Reactions

A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI50 values ranging from 0.569 to 16.6 µM and LC50 values ranging from 5.15 to >100 µM.

Effects of 13-hydroxy SM5887 in combination with other anticancer agents on human tumor cell lines

1996 ◽  
Vol 14 (4) ◽  
Author(s):  
Tatsuya Takagi ◽  
Yasuo Yazawa ◽  
Kenichi Suzuki ◽  
Yasuo Yamauchi ◽  
Yasuhiko Kano
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Synthesis and Biological Evaluation of New Piperazine Substituted 3, 5-Diarylisoxazolines

2019 ◽  
Vol 16 (2) ◽  
pp. 294-302 ◽  
Author(s):  
Hui Gao ◽  
Bei Liu ◽  
Ping Zhu ◽  
Li-Jun Zhang ◽  
Chun-Ping Wan ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Aim and Objective: Isoxazolines are an important class of nitrogen and oxygen-containing heterocycles, which have gained much importance as the potential biological agents. In order to study structureactivity relationships of isoxazolines, this work has been conducted. Materials and Methods: A series of new piperazine substituted 3, 5-diarylisoxazoline derivatives (6-31) were designed and synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anticancer effect against a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. Results: The substituents of the NH group of piperazine ring had an obvious influence on biological activities. Especially, compounds 5, 7, 8, 10, 11, 13 and 27-showed good inhibitory effect on the generation of NO compared to dexamethasone. Furthermore, derivatives 5, 6, 7, 8, 9, 13 and 26 were found to be potential selectively anticancer activity on human tumor cell lines, which displayed better cytotoxic activity to positive control 5- FU. Conclusion: Piperazine substituted 3, 5-diarylisoxazoline derivatives could be considered as new antiinflammatory and anticancer agents.

scholarly journals Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives

2016 ◽  
Vol 66 (1) ◽  
pp. 129-137 ◽  
Author(s):  
Paulo H. B. França ◽  
Edeildo F. Da Silva-Júnior ◽  
Pedro G. V. Aquino ◽  
Antônio E. G. Santana ◽  
Jamylle N. S. Ferro ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Human Tumor ◽  
Tetrazolium Salt ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Lead Compounds

Abstract Guanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies. In this study, we aimed at evaluating the cytotoxic effect of a series of synthetic guanylhydrazones. Different human tumor cell lines, by including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC50 values lower than 10 μmol L−1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents.

Heterobimetallic Ru(ii)/Fe(ii) complexes as potent anticancer agents against breast cancer cells, inducing apoptosis through multiple targets

Metallomics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 547-561 ◽  
Author(s):  
Adriana Pereira Mundim Guedes ◽  
Francyelli Mello-Andrade ◽  
Wanessa Carvalho Pires ◽  
Maria Alice Montes de Sousa ◽  
Paula Francinete Faustino da Silva ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Breast Cancer Cells ◽  
High Selectivity ◽  
Human Tumor ◽  
Chemotherapeutic Agents ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Antimetastatic Activity ◽  
New Chemotherapeutic Agents

Antimetastatic activity, high selectivity and cytotoxicity for human tumor cell lines make ruthenium(ii) complexes attractive for the development of new chemotherapeutic agents for cancer treatment.

Differential Increases in Glutathione S-Transferase Activities in a Range of Multidrug-Resistant Human Tumor Cell Lines

1989 ◽  
Vol 1 (6) ◽  
pp. 359-365 ◽  
Author(s):  
Richard D. H. Whelan ◽  
Louise K. Hosking ◽  
Alan J. Townsend ◽  
Kenneth H. Cowan ◽  
Bridget T. Hill
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Multidrug Resistant ◽  
Tumor Cell Lines ◽  
Glutathione S Transferase ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines
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