POTENT IN VITRO ANTICANCER ACTIVITIES OF RING-EXPANDED ("FAT") NUCLEOSIDES CONTAINING THE IMIDAZO[4,5-E][1,3]DIAZEPINE RING SYSTEM

The ring-expanded ("fat") nucleoside, 4,8-diamino-6-imino-6H-1-β-D-ribo- furanosylimidazo[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 d...

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Bibliographic Details
Published in:Nucleosides, nucleotides & nucleic acids nucleotides & nucleic acids, 2001-04, Vol.20 (4-7), p.1043-1045
Main Authors: Gill, Juliana K., Wang, Lijuan, Bretner, Maria, Newman, Rachel, Kyprianou, Natasha, Hosmane, Ramachandra S.
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Azepines - chemical synthesis
Azepines - pharmacology
Drug Screening Assays, Antitumor
Humans
Male
Nucleosides - pharmacology
Prostatic Neoplasms - drug therapy
Purine Nucleosides - chemical synthesis
Purine Nucleosides - pharmacology
Tumor Cells, Cultured
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Summary:The ring-expanded ("fat") nucleoside, 4,8-diamino-6-imino-6H-1-β-D-ribo- furanosylimidazo[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.
ISSN:1525-7770
1532-2335
DOI:10.1081/NCN-100002487