COMPLEXES OF STIGMASTEROL HEMIESTERS WITH L, D-TRYPTOPHAN

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68407700%3A21340%2F18%3A00323791" target="_blank" >RIV/68407700:21340/18:00323791 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

COMPLEXES OF STIGMASTEROL HEMIESTERS WITH L, D-TRYPTOPHAN

Popis výsledku v původním jazyce

Various biological activities of steroid compounds have been well known for decades now. Specific receptor binding assures selective distribution of radiolabelled steroid in the body. In this work we present synthesis of four conjugates of stigmasterol hemiesters with L,D-tryptophan and their complexes with platinum (II). Furthermore, we introduce preliminary results of labelling one of DOTA modified ligands with 68Ga. Debenzylation of prepared conjugates resulted in desired products (I - IV) in 74-88% yields. Platinum (II) complexes of obtained conjugates I - IV were prepared by a reaction of steroidal ligand with potassium tetrachloroplatinate in DMF. Steroidal ligand was modified by its reaction with a DOTA derivative in the presence of T3P. Labelling of obtained ligand with 68Ga was performed using eluate from 68Ge/68Ga generator in citrate buffer during 30 min at 80°C. Yield of radiolabelling (about 50%) was determined by HPLC.

Název v anglickém jazyce

COMPLEXES OF STIGMASTEROL HEMIESTERS WITH L, D-TRYPTOPHAN

Popis výsledku anglicky

Various biological activities of steroid compounds have been well known for decades now. Specific receptor binding assures selective distribution of radiolabelled steroid in the body. In this work we present synthesis of four conjugates of stigmasterol hemiesters with L,D-tryptophan and their complexes with platinum (II). Furthermore, we introduce preliminary results of labelling one of DOTA modified ligands with 68Ga. Debenzylation of prepared conjugates resulted in desired products (I - IV) in 74-88% yields. Platinum (II) complexes of obtained conjugates I - IV were prepared by a reaction of steroidal ligand with potassium tetrachloroplatinate in DMF. Steroidal ligand was modified by its reaction with a DOTA derivative in the presence of T3P. Labelling of obtained ligand with 68Ga was performed using eluate from 68Ge/68Ga generator in citrate buffer during 30 min at 80°C. Yield of radiolabelling (about 50%) was determined by HPLC.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

10402 - Inorganic and nuclear chemistry

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

2018

Kód důvěrnosti údajů

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