Design, synthesis and biological evaluation of rhein derivatives as anticancer agents

MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1812-1818 ◽  
Author(s):  
Junkai Huang ◽  
Zhuo Zhang ◽  
Peng Huang ◽  
Liqin He ◽  
Yong Ling
Keyword(s):  
Tumor Cell ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Promising Candidate ◽  
Design Synthesis ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.

Synthesis and biological evaluation of novel derivatives of gambogenic acid as anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.

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.

Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohan H. Patil ◽  
Uma D. Kabra ◽  
Krishna R. Gupta ◽  
Milind J. Umekar
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

Design, synthesis and biological evaluation of sulphonamide derivatives of benzofuran-imidazopyridines as anticancer agents

2021 ◽  
Vol 31 ◽  
pp. 100608
Author(s):  
Indraganti Sreenivasa Murthy ◽  
Reddymasu Sireesha ◽  
Kolli Deepti ◽  
P. Srinivasa Rao ◽  
R. Ramesh Raju
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

scholarly journals Design, Synthesis and Biological Evaluation of C-8 Modified Curcumol Derivatives as Potential Anticancer Agents

2021 ◽  
Author(s):  
Xiangwei Meng ◽  
Yingying Wei ◽  
Binglu Nong ◽  
Huajun Zhao ◽  
xingxian Zhang
Keyword(s):  
Cancer Cell ◽  
Anticancer Agents ◽  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Anti Cancer ◽  
Colorectal Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

Abstract A series of structural modification of curcumol derivatives at C-8 position were designed and synthesized, which structures were confirmed by 1H NMR,13C NMR and HRMS analysis. The tested compounds were evaluated for in vitro antitumor activity against colorectal cancer cell lines SW620, HCT116 and CaCo2. Many of the tested candidates exhibited higher inhibition efficiency than curcumol. Among them, compound 3l shows the best inhibitory effect on the viability of SW620 with IC50 value of 19.90 mM. The structure-activity relationships (SARs) of these derivatives were discussed, which showed that the introduction of amino or aryl groups tended to increase the anti-cancer activity. In addition, compound 3l may inhibit cancer cell proliferation through triggering cell apoptosis.

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of
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