Autor: Urban, M.; Kvasnica, M.; Dickinson, N. J.; Šarek, J.
Název práce v češtině: Biologicky aktivní triterpeny využitelné jako prodrugs
Název práce v angličtině: Biologically active triterpenoids usable as prodrugs
Klíčová slova v češtině: Triterpeny, prodrugs, cytotoxicita
Klíčová slova v angličtině: triterpenes, prodrugs,cytotoxicity
Abstrakt česky: Kapitola v knize se zabývá triterpeny s modifikovanými karboxylovými a hydroxylovými funkcemi, které by mohly sloužit jako prodrugs.
Abstrakt anglicky: Triterpenoids are a large group of natural compounds, many of which have interesting biological activities. Despite this, only a few derivatives are currently used as therapeutics. The main reason is that the active triterpenes usually have unfavorable pharmacological and physicochemical properties such as solubility and bioavailability. Therefore, many compounds with excellent activity in in vitro tests usually fail during clinical trial. Many research groups have tried to synthesize a variety of prodrugs in order to improve pharmacological properties of the active compound while retaining the desired biological activity. The most commonly chosen functional groups in triterpenes to be modified as prodrugs are hydroxyl and carboxyl. In this chapter, we are going to summarize all of the research that has been done in the area of triterpenoid prodrugs with the main focus on the modifications of hydroxyls and carboxyls. Commonly used types of prodrug groups (such as simple alkyl esters, other esters, ethers, amides etc.) will be shown as well as unusual prodrugs with more interesting biological and pharmacological properties (glycosides, hemi esters etc.). Their preparation will be shown as well as their chemical, biological, and pharmacological properties. In addition to this, we will compare each type of prodrug with the other prodrug types and will discuss their limits of use. Failures will be shown as well as successful compounds. In concluding, we will show prodrugs with the best properties as well as the current trends in the development of the new triterpenoid prodrugs including the most recent results from our research group.
Jazyk v originále: Anglický
Název knihy v originálním jazyce: Terpenoids and Squalene: Biosynthesis, Functions and Health Implications.
Typ publikace: Kapitola v knize: Terpenoids and Squalene: Biosynthesis, Functions and Health Implications.
Kód ISBN nebo ISMN: ISBN: 978-1-63463-656-8
Název nakladatele: Nova Science Publishers
Místo vydání: New York, USA
Strana od-do: 25-50
Celkový počet stran: 90
Způsob financování: Operational Program Research and Development for Innovations (project CZ.1.05/2.1.00/01.0030) and NPU I project LO1304 and from Ministry of Education, Youth and Sport of the Czech Republic and by the European Social Fund (CZ.1.07/2.3.00/30.0060)