| Autor: |
Tien Anh D; Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi 10000, Vietnam., Hai Nam N; Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi 10000, Vietnam., Kircher B; Immunobiology and Stem Cell Laboratory, Department of Internal Medicine V (Hematology and Oncology), Medical University Innsbruck, Anichstraße 35, 6020 Innsbruck, Austria.; Tyrolean Cancer Research Institute, Innrain 66, 6020 Innsbruck, Austria., Baecker D; Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Greifswald, Friedrich-Ludwig-Jahn-Straße 17, 17489 Greifswald, Germany. |
| Jazyk: |
angličtina |
| Zdroj: |
Molecules (Basel, Switzerland) [Molecules] 2023 Feb 19; Vol. 28 (4). Date of Electronic Publication: 2023 Feb 19. |
| DOI: |
10.3390/molecules28041973 |
| Abstrakt: |
In recent years, histone deacetylases (HDACs) have emerged as promising targets in the treatment of cancer. The approach is to inhibit HDACs with drugs known as HDAC inhibitors (HDACis). Such HDACis are broadly classified according to their chemical structure, e.g., hydroxamic acids, benzamides, thiols, short-chain fatty acids, and cyclic peptides. Fluorination plays an important role in the medicinal-chemical design of new active representatives. As a result of the introduction of fluorine into the chemical structure, parameters such as potency or selectivity towards isoforms of HDACs can be increased. However, the impact of fluorination cannot always be clearly deduced. Nevertheless, a change in lipophilicity and, hence, solubility, as well as permeability, can influence the potency. The selectivity towards certain HDACs isoforms can be explained by special interactions of fluorinated compounds with the structure of the slightly different enzymes. Another aspect is that for a more detailed investigation of newly synthesized fluorine-containing active compounds, fluorination is often used for the purpose of labeling. Aside from the isotope 19 F, which can be detected by nuclear magnetic resonance spectroscopy, the positron emission tomography of 18 F plays a major role. However, to our best knowledge, a survey of the general effects of fluorination on HDACis development is lacking in the literature to date. Therefore, the aim of this review is to highlight the introduction of fluorine in the course of chemical synthesis and the impact on biological activity, using selected examples of recently developed fluorinated HDACis. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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