Autor: Šidová, V.; Hodoň, J.; Urban M.
Název práce v češtině: Syntéza cytotoxicých derivátů triterpenů pomocí click reakcí
Název práce v angličtině: Synthesis of Cytotoxic Derivatives of Triterpenes Using Click Reaction
Klíčová slova v češtině: triterpeny, click reakce, cytotoxicita
Klíčová slova v angličtině:triterpenes, click reactions, cytotoxicity
Abstrakt česky: Pomocí click reakcí byla syntetizována skupina triterpenů modifikována v poloze C-30
Abstrakt anglicky: Triterpenes are natural compounds abundant in plants and a lot of them are selectively cytotoxic on many cancer cell lines, including resistant.1 Despite that, their use is rather limited by inappropriate pharmacological properties. We used azide-alkyne Huisgen cycloaddition to modify the triterpenoid skeleton in the position 30. We connected azides 9, 11, 10, and 12 to other molecules such as heterocycles amines etc. in order to increase their IC50 and solubility in water based media. The method is versatile and beside small molecules, active terpenes were connected to cholic acids that may serve as a second pharmacophore and may improve adsorption of the resulting conjugates from intestine. To sum up, 46 new compounds were prepared and their biological properties, such as cytotoxicity and ADME-TOX properties are currently being evaluated. Preliminary data show increase of the IC50 in comparison to the starting terpenes.
Jazyk v originále: Anglický
Publikace abstraktu: 141/166
Forma prezentace: poster
Název konference: Advances in Organic, Bioorganic, and Pharmaceutical Chemistry „Liblice 2015“
Místo konání: Olomouc (Czech Republic)
Datum konání: November 6-8
Rok konání: 2015
Způsob financování: GACR Reg. No.15-05620S