Synthesis of novel 2, 5-dihydrofuran derivatives and evaluation of their anticancer activity

According to metal-catalyzed [3 + 2] cycloaddition reaction, we synthesized a series of novel 2, 5-dihydrofuran derivatives and evaluated their in vitro anti-cancer activities via MTT method. The bioassay showed that the majority of the resultant compounds exerted anti-tumor effect against four huma...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2012-02, Vol.48, p.69-80
Main Authors: Zhang, Yikai, Zhong, Hanyu, Wang, Tiantian, Geng, Dongping, Zhang, Mingfeng, Li, Ke
Format: Article
Language:English
Subjects:
2, 5-Dihydrofuran derivatives
Anti-cancer activity
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Survival - drug effects
Crystal structure
Furans - chemical synthesis
Furans - chemistry
Furans - pharmacology
General aspects
HeLa Cells
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Medical sciences
Metal-catalyzed cycloaddition reaction
Models, Molecular
Pharmacology. Drug treatments
Spectrometry, Mass, Electrospray Ionization
Spectrophotometry, Infrared
Structure-Activity Relationship
Synthesis
X-Ray Diffraction
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Summary:According to metal-catalyzed [3 + 2] cycloaddition reaction, we synthesized a series of novel 2, 5-dihydrofuran derivatives and evaluated their in vitro anti-cancer activities via MTT method. The bioassay showed that the majority of the resultant compounds exerted anti-tumor effect against four human cancer cell lines to various extents, which supported the rationale of the design. Compounds 9e and 10g showed the highest activity with broad anti-cancer spectrum, which were good candidates for further evaluation. [Display omitted] ► We synthesized a series of novel 2, 5-dihydrofuran derivatives. ► Metal-catalyzed [3 + 2] cycloaddition reaction was employed. ► We determine the reaction mediate via X-ray crystallography. ► All resultant compounds were evaluated for their in vitro cytotoxic activities. ► The result shows some of resultant compounds have potential anti-cancer activity.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2011.11.036