BIBLIOS

Tipo
Artigos em Revista

Tipo de Documento
Artigo Completo

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

Participantes na publicação
S. Schwarz (Author)
B. Siewert (Author)
R. Csuk (Author)
A. P. Rauter (Author)
Dep. Química e Bioquímica
CQB

Resumo
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.


Instituição
FACULDADE DE CIÊNCIAS DA UNIVERSIDADE DE LISBOA

Suporte
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identificadores da Publicação
ISSN - 0223-5234

Editora
Elsevier BV



Identificadores do Documento
DOI - https://doi.org/10.1016/j.ejmech.2014.11.019
URL - http://dx.doi.org/10.1016/j.ejmech.2014.11.019

Identificadores de Qualidade
Web Of Science Q1 (2018) - 4.833 - Medicinal Chemistry

Anotações
I am the corresponding author

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