Home Neoplasma 2009 Neoplasma Vol.56, No.3, p.177-186, 2009

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Founded: 1954
ISSN 0028-2685
ISSN 1338-4317 (online)

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Neoplasma Vol.56, No.3, p.177-186, 2009

Title: Cytarabine conjugates with biologically active molecules and their potential anticancer activity
Author: L. NOVOTNY, P. RAUKO

Abstract: The presented review article deals with various conjugates of arabinosylcytosine (araC). This powerful drug that is routinely used in therapy of hematological malignancies has some shortcomings, which limit its use and therapeutic effects. These are low lipophilicity, low stability to degrading enzymes and need for biological activation through phosphorylation. Conjugating araC to another molecule is done with the intention of increasing araC stability and lipophilicity and possibly avoiding rate-limiting araC phosphorylation. An attachment of that another molecule, possessing its own biological activity, may result in formation of a conjugated molecule with new biological activities and better therapeutic potential. The review deals with various araC conjugates formed at the positions N4, 2, 2’, 3’ and 5’. Biological activities and differences from araC of compounds formed by conjugation are also discussed.

Keywords: Cytarabine, arabinosylcytosine, conjugates, biologic activity, anticancer activity
Year: 2009, Volume: 56, Issue: 3 Page From: 177, Page To: 186
doi:10.4149/neo_2009_03_177


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