Preparation of Hydrazones of R- and S-usnic Acid Their Antitumor Activity

České info

PRÍPRAVA A PROTINÁDOROVÉ ÚČINKYACYLHYDRAZÓNOV R R- A S S-USNOVEJKYSELINY

Hydrazóny kyseliny R- a S-usnovej sa pripravili kondenzáciou príslušného enantiomeru kyselinyusnovej a hydrazidov aromatických kyselín. Získané látky sa charakterizovali spektrálnymi metó-dami, kinetika reakcie sa sledovala micelárnou elektrokinetickou chromatografiou, enantiomernačistota pripravených látok sa potvrdila kapilárnou elektroforézou v prítomnosti g-cyklodextrínu.Pripravené hydrazóny sa hodnotili ako potenciálne antimitotiká. Protinádorová aktivita sa sledo-vala na línii ľudských nádorových buniek; celková aktivita hodnotených látok bola nízka, aleR-enantiomery boli aktívnejšie ako ich stereoizoméry.

Klíčová slova:
R-, S-usnová kyselina – hydrazóny – MEKC – antimitotická aktivita –protinádorová aktivita

Authors: B. Proksa; A. Proksová
Authors‘ workplace: Slovakofarma, a. s., Hlohovec
Published in: Čes. slov. Farm., 1999; , 233-236
Category:

Overview

Hydrazones of R- and S-usnic acid were prepared by condensation of the appropriate enantiomer ofusnic acid with hydrazides of aromatic acids. Prepared compounds were characterized by spectralmethods. Reaction kinetic was studied with capillary electrokinetic chromatography, enantiomericpurity of products was checked by capillary electrophoresis in the presence of g-cyclodextrin.Obtained hydrazones were tested as prospective antimitotic agents. The antitumor activity wasscreened in vitro on human tumor cell lines. The overall activity of tested compounds was low,however, the R- enantiomers were more active than their opposite stereoisomers.

Key words:
R-, S-usnic acid – hydrazones – MEKC – antimitotic activity – antitumor activity

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