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6th Internet World Congress for Biomedical Sciences

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New bicyclic non-condensited thiazolidones-4 and their cytostatic activity

Yaryna Shparhala(1), Vladimir Muzichenco(2), Boris Zimenkovsky(3)
(1)(2)(3)Department of Pharmaceutical, Org. and Bioorg. Chemistry. Danylo Halytsky Lviv Medical University - Lviv. Ukraine

Discussion Board Contact address: Yaryna Shparhala
Department of Pharmaceutical, Org. and Bioorg. Chemistry Danylo Halytsky Lviv Medical University
69, Pekarska St. Lviv
Lviv 290010 Ukraine
yaryna@sade.com
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ABSTRACT

The search of new cytostatic drugs is one of the most actual problems of the modern medicine. Therefore the reseach of cytostatic activity of thiazolidones-4 has got great prospect. Our aim was to find the new biological active substances of such type. As a result we obtained the bicyclic non-condensated thiazolidones-4 (I, II, III) on the base of 1,5-diamino-3-azapentane and 1,5-diamino-3-oxapentane:

We have learnt the influence of our substances on the proliferation of mises’ subnormal fibroblasts (line NIH-3T3) and human lungs adenocarcinoma cells (line A-549). We determined the effect of substances by the quantity 3H-timidine included.

The introduction of our substances (concentration 1*10-5 moll/l) in the adenocarcinoma human lungs cells culture and mises’ subnormal fibroblasts culture had caused strong decrease of including of 3H-timidine in DNA. All of these substances are effective in 2*10-5 moll/l concentrations. The most effective substances are: #55 (1,5 bis-(2-thioxo–4–oxo-5-vanilydenethiazolidine–3-yl)–3-oxapentane) and #73 (1,5 bis-(2-thioxo-4–oxo-5-vanilydenethiazolidine-3-yl)–3-thiocarboxy-3-azapentane). We compared the cytostatic activity of our substances #55 and #73 (concentration 2*10-5 moll/l) with known cytostatic drugs such as Lomustin, Endoxan, Paclitaxel and Cysplatin. These substances (as we see from the graph) have a highly effective cytostatic contact activity on the cancer cells. These results are the reason for the further investigations.
Keywords: thiazolidones-4 - cytostatic activity - adenocarcinoma cells -
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[Pharmacology]
Next: Differential effects of 18-Methoxycoronaridine (18-MC) on the behavioural and neurochemical responses to chronic cocaine and morphine: Implications for sensitization in the mediation of drug addiction
Yaryna Shparhala, Vladimir Muzichenco, Boris Zimenkovsky
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