New polyfluorothiopropanoyloxy derivatives of 5 beta-cholan-24-oic acid designed as drug absorption modifiers

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F13%3A33148057" target="_blank" >RIV/61989592:15310/13:33148057 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/62157124:16370/13:43872230 RIV/60461373:22340/13:43895075 RIV/60461373:22330/13:43895075 RIV/60461373:22810/13:43895075

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0039128X13001220" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0039128X13001220</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.steroids.2013.05.012" target="_blank" >10.1016/j.steroids.2013.05.012</a>

Jazyk výsledku

angličtina

Název v původním jazyce

New polyfluorothiopropanoyloxy derivatives of 5 beta-cholan-24-oic acid designed as drug absorption modifiers

Popis výsledku v původním jazyce

A series of final six propanoyloxy derivatives of 5 beta-cholan-24-oic acid (tridecafluoroctylsulfanyl- and tridecafluoroctylsulfinylethoxycarbonylpropanoyloxy derivatives) as potential drug absorption promoters (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplished by H-1 NMR, C-13 NMR, IR and MS spectroscopy methods. All the prepared compounds were analyzed using RP-TLC, and their lipophilicity (R-M) was determined. The hydrophobicity (log P), solubility (log S), polar surface area (PSA) and molar volume (MV) of the studied compounds were also calculated. All the target compounds were tested for their in vitro transdermal penetration effectand as potential intestinal absorption enhancers. The cytotoxicity of all the evaluated compounds was evaluated against normal human skin fibroblast cells. Their anti-proliferative activity was also assessed against human cancer cell lin

Název v anglickém jazyce

New polyfluorothiopropanoyloxy derivatives of 5 beta-cholan-24-oic acid designed as drug absorption modifiers

Popis výsledku anglicky

A series of final six propanoyloxy derivatives of 5 beta-cholan-24-oic acid (tridecafluoroctylsulfanyl- and tridecafluoroctylsulfinylethoxycarbonylpropanoyloxy derivatives) as potential drug absorption promoters (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplished by H-1 NMR, C-13 NMR, IR and MS spectroscopy methods. All the prepared compounds were analyzed using RP-TLC, and their lipophilicity (R-M) was determined. The hydrophobicity (log P), solubility (log S), polar surface area (PSA) and molar volume (MV) of the studied compounds were also calculated. All the target compounds were tested for their in vitro transdermal penetration effectand as potential intestinal absorption enhancers. The cytotoxicity of all the evaluated compounds was evaluated against normal human skin fibroblast cells. Their anti-proliferative activity was also assessed against human cancer cell lin

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Steroids

ISSN

0039-128X

e-ISSN

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Svazek periodika

78

Číslo periodika v rámci svazku

9

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

13

Strana od-do

832-844

Kód UT WoS článku

000322934700006

EID výsledku v databázi Scopus

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