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Broxuridine

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Ivan Butula – 1st expert on this subject based on the ideXlab platform

  • macromolecular prodrugs v polymer Broxuridine conjugates
    International Journal of Pharmaceutics, 1995
    Co-Authors: Branka Zorc, Dusica Maysinger, Igor Kalcic, Ivan Butula

    Abstract:

    Abstract Broxuridine (BrdU) was covalently bound to α,β-poly[(2-hydroxyethyl)- dl -aspartamide](PHEA) and α,β-poly[(2-aminoethyl)-DL-aspartamide]-α,β-poly[(2-hydroxyethyl)-DL-aspartamide](PAHA). BrdU was first chemically modified to 3′- O -acetyl-5′- O -chloroformyl-5-bromo-2′-deoxyuridine (AcCBrdU) and 3′- O -acetyl-5′- O -phosphooxydichloride-5-bromo-2′-deoxyuridine (AcPBrdU). These compounds were bound to PHEA by carbonate and phosphodiester linkages, respectively. 5-Bromo-2′-deoxyuridine 5′-monophosphate (PBrdU) was linked to PAHA by an amide type bond. Neuroepithelial cells were used as a model system to assess the suitability of the conjugated BrdU for cell proliferation. Parallel experiments were performed with unconjugated BrdU and the extent of incorporation into DNA was determined by immunocytochemistry using an BrdU antibody. The results from these studies suggest that conjugated BrdU can be used as an alternative to currently used means of BrdU delivery.

Branka Zorc – 2nd expert on this subject based on the ideXlab platform

  • macromolecular prodrugs v polymer Broxuridine conjugates
    International Journal of Pharmaceutics, 1995
    Co-Authors: Branka Zorc, Dusica Maysinger, Igor Kalcic, Ivan Butula

    Abstract:

    Abstract Broxuridine (BrdU) was covalently bound to α,β-poly[(2-hydroxyethyl)- dl -aspartamide](PHEA) and α,β-poly[(2-aminoethyl)-DL-aspartamide]-α,β-poly[(2-hydroxyethyl)-DL-aspartamide](PAHA). BrdU was first chemically modified to 3′- O -acetyl-5′- O -chloroformyl-5-bromo-2′-deoxyuridine (AcCBrdU) and 3′- O -acetyl-5′- O -phosphooxydichloride-5-bromo-2′-deoxyuridine (AcPBrdU). These compounds were bound to PHEA by carbonate and phosphodiester linkages, respectively. 5-Bromo-2′-deoxyuridine 5′-monophosphate (PBrdU) was linked to PAHA by an amide type bond. Neuroepithelial cells were used as a model system to assess the suitability of the conjugated BrdU for cell proliferation. Parallel experiments were performed with unconjugated BrdU and the extent of incorporation into DNA was determined by immunocytochemistry using an BrdU antibody. The results from these studies suggest that conjugated BrdU can be used as an alternative to currently used means of BrdU delivery.

Igor Kalcic – 3rd expert on this subject based on the ideXlab platform

  • macromolecular prodrugs v polymer Broxuridine conjugates
    International Journal of Pharmaceutics, 1995
    Co-Authors: Branka Zorc, Dusica Maysinger, Igor Kalcic, Ivan Butula

    Abstract:

    Abstract Broxuridine (BrdU) was covalently bound to α,β-poly[(2-hydroxyethyl)- dl -aspartamide](PHEA) and α,β-poly[(2-aminoethyl)-DL-aspartamide]-α,β-poly[(2-hydroxyethyl)-DL-aspartamide](PAHA). BrdU was first chemically modified to 3′- O -acetyl-5′- O -chloroformyl-5-bromo-2′-deoxyuridine (AcCBrdU) and 3′- O -acetyl-5′- O -phosphooxydichloride-5-bromo-2′-deoxyuridine (AcPBrdU). These compounds were bound to PHEA by carbonate and phosphodiester linkages, respectively. 5-Bromo-2′-deoxyuridine 5′-monophosphate (PBrdU) was linked to PAHA by an amide type bond. Neuroepithelial cells were used as a model system to assess the suitability of the conjugated BrdU for cell proliferation. Parallel experiments were performed with unconjugated BrdU and the extent of incorporation into DNA was determined by immunocytochemistry using an BrdU antibody. The results from these studies suggest that conjugated BrdU can be used as an alternative to currently used means of BrdU delivery.