Abstract
Thioflavone derivatives are the thio analogs of the core constituent of the natural product class of flavones. Based on the position and oxidation level of sulfur, they can be divided into three major categories: 4-thioflavones, 1-thioflavones and 1-thioflavones 1,1-dioxide. In recent years, great efforts have been made to develop an approach for the synthesis of thioflavones, especially 1- thioflavones with high functional group compatibility, high yields, low toxicity as well as proceeding under a mild condition, and a variety of synthetic protocols have been developed, the method of choice being dependent on the nature of substrates. As isosteric analogs of biologically active flavones, thioflavones also exhibit various pharmaceutical properties, such as antimicrobial, anticancer and neuroprotective activities. Replacement of the oxygen atom on flavone skeleton by a sulfur atom resulted in modified biological effects due in most part to the change of the structural properties. However, these varying effects depend on the substituents present and the test species. To provide a comprehensive vision of this class of compounds, this review primarily focuses on the structure, synthetic methods, biological properties as well as structure-activity relationships of thioflavones.
Keywords: Anticancer, antimicrobial, thiochromone, thioflavone, neuroprotective, SARs.
Mini-Reviews in Medicinal Chemistry
Title:The Chemistry and Biological Effects of Thioflavones
Volume: 18 Issue: 20
Author(s): Jinyun Dong, Qijing Zhang, Qingqing Meng, Zengtao Wang, Shaoshun Li*Jiahua Cui*
Affiliation:
- School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai,China
- School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai,China
Keywords: Anticancer, antimicrobial, thiochromone, thioflavone, neuroprotective, SARs.
Abstract: Thioflavone derivatives are the thio analogs of the core constituent of the natural product class of flavones. Based on the position and oxidation level of sulfur, they can be divided into three major categories: 4-thioflavones, 1-thioflavones and 1-thioflavones 1,1-dioxide. In recent years, great efforts have been made to develop an approach for the synthesis of thioflavones, especially 1- thioflavones with high functional group compatibility, high yields, low toxicity as well as proceeding under a mild condition, and a variety of synthetic protocols have been developed, the method of choice being dependent on the nature of substrates. As isosteric analogs of biologically active flavones, thioflavones also exhibit various pharmaceutical properties, such as antimicrobial, anticancer and neuroprotective activities. Replacement of the oxygen atom on flavone skeleton by a sulfur atom resulted in modified biological effects due in most part to the change of the structural properties. However, these varying effects depend on the substituents present and the test species. To provide a comprehensive vision of this class of compounds, this review primarily focuses on the structure, synthetic methods, biological properties as well as structure-activity relationships of thioflavones.
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Cite this article as:
Dong Jinyun , Zhang Qijing , Meng Qingqing, Wang Zengtao , Li Shaoshun*, Cui Jiahua *, The Chemistry and Biological Effects of Thioflavones, Mini-Reviews in Medicinal Chemistry 2018; 18 (20) . https://dx.doi.org/10.2174/1389557518666180515145633
DOI https://dx.doi.org/10.2174/1389557518666180515145633 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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