Potent in vitro anticancer activities of ring-expanded ("fat") nucleosides containing the imidazo[4,5-E][1,3]diazepine ring system

Juliana K. Gill, Lijuan Wang, Maria Bretner, Rachel Newman, Natasha Kyprianou, Ramachandra S. Hosmane

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

The ring-expanded ("fat") nucleoside, 4,8-diamino-6-imino-6H-1-β-D-ribofuranosylimidazo[4,5-e][1,3]diazepine (1) and its 2′,3′,5′-tri-O-benzoyl derivative (2) exhibited potent broad spectrum anticancer activities in vitro against a wide variety of human tumor cell lines. The tribenzoyl derivative 2 was found to be considerably more active than the parent nucleoside 1. Further studies using human prostate cancer cells PC-3 and DU-145 suggest that the treatment of exponentially growing culture cells with 1 and 2 leads to marked loss of cell viability in a dose-dependent manner.

Original languageEnglish
Pages (from-to)1043-1045
Number of pages3
JournalNucleosides, Nucleotides and Nucleic Acids
Volume20
Issue number4-7
DOIs
StatePublished - 2001
Externally publishedYes

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