BIBLIOS

Document type
Journal articles

Document subtype
Full paper

Title
New antitumor 6-chloropurine nucleosides inducing apoptosis and G2/M cell cycle arrest

Participants in the publication
S. Schwarz (Author)
B. Siewert (Author)
R. Csuk (Author)
A. P. Rauter (Author)
Dep. Química e Bioquímica
CQB

Summary
Treating cancer has been challenging for decades, following countless approaches and attempts. Nucleosides, alone or as part of nucleotides, are vital elements of living systems and have shown pharmacological effects, e.g. as antibiotic or antiviral agents. We investigated the antitumor potential on human melanoma, lung and ovarian carcinomas, and on colon adenocarcinoma of a new series of purine nucleosides based on a 6-chloropurine or a 2-acetamido-6-chloropurine scaffold linked to perbenzylated hexosyl (glucosyl, galactosyl and mannosyl) residues. All compounds were tested in a sulforhodamine B (SRB) assay for their cytotoxicity and provided micromolar GI50 values with order of magnitude comparable to structurally similar chemotherapeutics, namely 2-chloro-2′-deoxyadenosine (cladribine). Furthermore, the induction of apoptosis was established and cell cycle analysis was accomplished demonstrating a G2/M cell cycle arrest.


Institution
FACULDADE DE CIÊNCIAS DA UNIVERSIDADE DE LISBOA

Where published
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Publication Identifiers
ISSN - 0223-5234

Publisher
Elsevier BV



Document Identifiers
DOI - https://doi.org/10.1016/j.ejmech.2014.11.019
URL - http://dx.doi.org/10.1016/j.ejmech.2014.11.019

Rankings
Web Of Science Q1 (2018) - 4.833 - Medicinal Chemistry

Notes
I am the corresponding author

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