synthesis and biological evaluation of novel 1′-branched and spironucleosides analogues

1
2005 Nucleic acids U 0700 Synthesis and Biological Evaluation of Novel 1'-Branched and Spironucleosides Analogues. — The anionic reactivity of the cyano function and especially the addition of organolithium reagents both to protected bromo uridine and 2'-deoxy uridine deriv- atives is investigated as well as the antiviral and antitumoral activity of some of the new anomeric spironucleosides and of 2',3'-didehydro-2',3'-dideoxy nucleoside (IX), a structural analogue of known anti-HIV agents. None of the compounds reveals antiviral activity, however, spironucleoside (IV) and didehydronucleoside (IX) display cytostat- ic activity against murine leukemia and human T-lymphocyte cells. — (CHATGILIALOGLU, C.; FERRERI, C.; GIMISIS*, T.; ROBERTI, M.; BALZARINI, J.; DE CLERCQ, E.; Nucleosides, Nucleotides Nucleic Acids 23 (2004) 10, 1565-1581; Lab. Org. Chem., Univ. Athens, GR-15771 Athens, Greece; Eng.) — H. Hoennerscheid 20- 203

Upload: chryssostomos-chatgilialoglu

Post on 06-Jun-2016

215 views

Category:

Documents


2 download

TRANSCRIPT

Page 1: Synthesis and Biological Evaluation of Novel 1′-Branched and Spironucleosides Analogues

2005

Nucleic acidsU 0700 Synthesis and Biological Evaluation of Novel 1'-Branched and Spironucleosides

Analogues. — The anionic reactivity of the cyano function and especially the addition of organolithium reagents both to protected bromo uridine and 2'-deoxy uridine deriv-atives is investigated as well as the antiviral and antitumoral activity of some of the new anomeric spironucleosides and of 2',3'-didehydro-2',3'-dideoxy nucleoside (IX), a structural analogue of known anti-HIV agents. None of the compounds reveals antiviral activity, however, spironucleoside (IV) and didehydronucleoside (IX) display cytostat-ic activity against murine leukemia and human T-lymphocyte cells. — (CHATGILIALOGLU, C.; FERRERI, C.; GIMISIS*, T.; ROBERTI, M.; BALZARINI, J.; DE CLERCQ, E.; Nucleosides, Nucleotides Nucleic Acids 23 (2004) 10, 1565-1581; Lab. Org. Chem., Univ. Athens, GR-15771 Athens, Greece; Eng.) — H. Hoennerscheid

20- 203