Wyniki wyszukiwania

1

The effect of introduction of a formamidino group to the molecule of doxorubicin on its biological properties

100%

Kik K., Studzian K., Lukawska M., Oszczapowicz I., Szmigiero L.

Acta Biochimica Polonica

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2007

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tom 54

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nr Supplement 4

2

New daunorubicin analogue — studies on the mechanism of cytotoxicity

100%

Ciesielka E., Studzian K., Wasowska M., Oszczapowicz I., Szmgiero L.

Acta Biochimica Polonica

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2003

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tom 50

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nr Supplement 1

3

Cytotoxicity and inhibitory properties against topoisomerase II of doxorubicin and its formamidine derivatives

100%

Kik K., Studzian K., Wasowska-Lukawska M., Oszczapowicz I., Szmigiero L.

Acta Biochimica Polonica

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2009

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tom 56

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nr 1

135-142

This work was undertaken to compare cytotoxicity, DNA damaging properties and effect on DNA cleavage by topoisomerase II of the anthracycline drug doxorubicin (DOX) and its two derivatives with a formamidino group containing a cyclic amine moiety such as morpholine (DOXM) or hexamethyleneimine (DOXH). The tetrazolium dye colorimetric assay was used to determine the cytotoxic activity of anthracyclines toward L1210 leukemia cells. DNA damage was measured by alkaline elution technique. The effect of anthracyclines on DNA cleavage was studied in a cell-free system containing supercoiled pBR322 DNA and purified human topoisomerase II. The cytotoxicity data and the results of studies on the mechanism of DNA break formation by anthracyclines at the cellular level and in the cell-free system showed that the presence of the formamidino group in the doxorubicin molecule reduced its ability to stimulate DNA cleavage by DNA topoisomerase II. Conclusion: DNA topoisomerase II is not a primary cellular target for DOXM or DOXH. An advantageous feature of formamidinoanthracyclines is their mechanism of cytotoxic action which is not related to the inhibition of DNA topoisomerase II. Therefore this class of anthracyclines seems to be a good source for selection of an anticancer drug directed toward cancer cells with the developed multidrug resistance attributed to the presence of altered DNA topoisomerase II.

4

Interactions of novel morpholine and hexamethylene derivatives of anthracycline antibiotics

86%

Wilmanska D., Piestrzeniewicz K., Studzian K., Wasowska M., Oszczapowicz I., Gniazdowski M.

Acta Biochimica Polonica

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2003

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tom 50

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nr Supplement 1

5

The ability of new formamidine sugar-modified derivatives of daunorubicin to stimulate free radical formation in three enzymatic systems: NADH dehydrogenase, NADPH cytochrome p450 reductase and xanthine oxidase

86%

Pawlowska J., Tarasiuk J., Borowski E., Wasowska M., Oszczapowicz I., Wolf C. R.

Acta Biochimica Polonica

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2000

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tom 47

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nr 1

Some sterically hindered N-substituted derivatives of daunorubicin are known to be poor substrates for NADH dehydrogenase, NADPH cytochrome P450 reductase and xanthine oxidase. In consequence, poor oxygen radical generation by these compounds is observed. In this study we examined a new family of sugar-N-substituted derivatives of daunorubicin bearing a bulky substituent introduced on the nitrogen atom through the amidine spacer. These compounds were found to be very active in radical formation catalyzed by all three studied enzymes. Thus, the introduction of a heterocyclic ring, even if it is bulky but flexible, on the nitrogen atom of daunosamine moiety through the one-atom spacer (amidine group), does not induce the steric hindrance effect on the interaction of daunorubicin derivatives with these flavoprotein enzymes.

Ograniczanie wyników

5 Acta Biochimica Polonica

5 Oszczapowicz I.

4 Studzian K.

3 Wasowska M.

2 Kik K.

2 Szmigiero L.

1 Borowski E.

1 Ciesielka E.

1 Gniazdowski M.

1 Lukawska M.

1 Pawlowska J.

1 Piestrzeniewicz K.

1 Szmgiero L.

1 Tarasiuk J.

1 Wasowska-Lukawska M.

1 Wilmanska D.

1 Wolf C. R.

1 2009

1 2007

2 2003

1 2000

The effect of introduction of a formamidino group to the molecule of doxorubicin on its biological properties

New daunorubicin analogue — studies on the mechanism of cytotoxicity

Cytotoxicity and inhibitory properties against topoisomerase II of doxorubicin and its formamidine derivatives

Interactions of novel morpholine and hexamethylene derivatives of anthracycline antibiotics

The ability of new formamidine sugar-modified derivatives of daunorubicin to stimulate free radical formation in three enzymatic systems: NADH dehydrogenase, NADPH cytochrome p450 reductase and xanthine oxidase