Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells

Amin, Kamelia M.; Abou‐Seri, Sahar M.; Awadallah, Fadi M.; Eissa, Amal A.M.; Hassan, Ghada S.; Abdulla, Mohamed M.

doi:10.1016/j.ejmech.2014.11.027

Cited by 52 publications

(17 citation statements)

References 49 publications

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“…Both of these derivatives were N-1 unsubstituted. Overall, the structure activity relationships suggested that the activity was influenced by the substitution pattern on pyrazoline ring [58]. Amin et al synthesized two groups of phenylsulfonyl and sulfamoylphenyl coumarin based pyrazoline hybrids.…”

Section: Clinical Drug-pyrazoline Hybridsmentioning

confidence: 99%

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Matiadis

Sagnou

2020

IJMS

104

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Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens. They have attracted significant attention from organic and medicinal chemists due to their potent biological activities and the numerous possibilities for structural diversification. In the last decade, they have been intensively studied as targets for potential anticancer therapeutics, producing a steady yearly rise in the number of published research articles. Many pyrazoline derivatives have shown remarkable cytotoxic activities in the form of heterocyclic or non-heterocyclic based hybrids, such as with coumarins, triazoles, and steroids. The enormous amount of related literature in the last 5 years prompted us to collect all these published data from screening against cancer cell lines, or protein targets like EGFR and structure activity relationship studies. Therefore, in the present review, a comprehensive account of the compounds containing the pyrazoline nucleus will be provided. The chemical groups and the structural modifications responsible for the activity will be highlighted. Moreover, emphasis will be given on recent examples from the literature and on the work of research groups that have played a key role in the development of this field.

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Section: Clinical Drug-pyrazoline Hybridsmentioning

confidence: 99%

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Matiadis

Sagnou

2020

IJMS

104

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“…Among the reported activities, it is important to note that pyrazolines are not only useful in treatment of various cancer types, including brain, bone, mouth, esophagus, stomach, liver, bladder, pancreas, cervix, lung, breast, colon, rectum, and prostate cancers, but also some of them act as cancer chemopreventive agents [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23]. In many studies, pyrazoline derivatives were reported as epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors [19], aurora kinase inhibitors [20], COX-2/B-Raf inhibitors [21], telomerase inhibitors [22], tubulin assembling inhibitors [23]. Additionally, 1,3,4-oxadiazole has emerged as an important scaffold owing to its metabolic profile and ability to engage in hydrogen bonding with receptor site.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents

et al. 2015

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New pyrazoline derivatives were synthesized and evaluated for their cytotoxic effects on AsPC-1 human pancreatic adenocarcinoma, U87 and U251 human glioblastoma cell lines. 1-[((5-(4-Methylphenyl)-1,3,4-oxadiazol-2-yl)thio)acetyl]-3-(2-thienyl)-5-(4-chlorophenyl)-2-pyrazoline (11) was found to be the most effective anticancer agent against AsPC-1 and U251 cell lines, with IC50 values of 16.8 µM and 11.9 µM, respectively. Tumor selectivity of compound 11 was clearly seen between Jurkat human leukemic T-cell line and human peripheral blood mononuclear cells (PBMC). Due to its promising anticancer activity, compound 11 was chosen for apoptosis/necrosis evaluation and DNA-cleavage analysis in U251 cells. Compound 11-treated U251 cells exhibited apoptotic phenotype at low concentration (1.5 µM). DNA-cleaving efficiency of this ligand was more significant than cisplatin and was clearly enhanced by Fe(II)-H2O2-ascorbic acid systems. This result pointed out the relationship between the DNA cleavage and the cell death.

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“…Different substitutions of chroman produce a large number of derivatives. Among them, 2‐phenylchroman‐4‐one derivatives ( 15 ‐ 18 ) are the most important ones . Because they are effective in inhibiting dyskerin, they are thought to inhibit the interaction of dyskerin and NOP10 and reduce telomerase activity .…”

Section: Small Molecule Inhibitorsmentioning

confidence: 99%

Therapeutic strategies for targeting telomerase in cancer

Chen

Tang

Shi

et al. 2019

Medicinal Research Reviews

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Telomere and telomerase play important roles in abnormal cell proliferation, metastasis, stem cell maintenance, and immortalization in various cancers. Therefore, designing of drugs targeting telomerase and telomere is of great significance. Over the past two decades, considerable knowledge regarding telomere and telomerase has been accumulated, which provides theoretical support for the design of therapeutic strategies such as telomere elongation. Therefore, the development of telomere‐based therapies such as nucleoside analogs, non‐nucleoside small molecules, antisense technology, ribozymes, and dominant negative human telomerase reverse transcriptase are being prioritized for eradicating a majority of tumors. While the benefits of telomere‐based therapies are obvious, there is a need to address the limitations of various therapeutic strategies to improve the possibility of clinical applications. In this study, current knowledge of telomere and telomerase is discussed, and therapeutic strategies based on recent research are reviewed.

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Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells

Cited by 52 publications

References 49 publications

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents

Therapeutic strategies for targeting telomerase in cancer

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