scholarly journals Inhibitory effects of acyclic nucleoside phosphonate analogs, including (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, on Epstein-Barr virus replication.

1991 ◽  
Vol 35 (11) ◽  
pp. 2440-2443 ◽  
Author(s):  
J C Lin ◽  
E De Clercq ◽  
J S Pagano
1998 ◽  
Vol 9 (3) ◽  
pp. 275-282 ◽  
Author(s):  
A Meerbach ◽  
A Holý ◽  
P Wutzler ◽  
E De Clercq ◽  
J Neyts

The anti-Epstein–Barr virus (EBV) activity of different classes of compounds was assessed by means of an EBV DNA hybridization assay using a digoxigenin-labelled probe specific for the BamHI W fragment of the EBV genome, as well as by measuring viral capsid antigen (VCA) expression after a 7 day incubation period of P3HR-1 producer cells with the test substances. Acyclovir, ganciclovir, cidofovir and zidovudine were included as reference compounds. Several compounds proved to be potent and selective inhibitors of EBV DNA synthesis and VCA expression. Of the new compounds that were evaluated for their anti-EBV activity, the highest efficacy (lowest EC50) and highest selectivity index (SI) were shown by the purine nucleoside analogue 2-amino-7-[(1,3-dihydroxy-2-propoxy)methyl]purine (S2242) (EC50 0.6 ng/ml; SI 600), the acyclic nucleoside phosphonate analogues 9-(2-phosphonomethoxyethyl)-6-dimethylaminopurine (EC50 1.1 μg/ml; SI 91), 9-(2-phosphonomethoxyethyl)-2-amino-6-benzhydrylaminopurine (EC501.3 μg/ml; SI 29), 7-(2-phosphonomethoxyethyl)-6-dimethylaminopurine (EC50 0.8 μg/ml; SI 56), 9-( R)-(2-phosphonomethoxypropyl)-6-(2-dimethylaminoethyl)-aminopurine (EC50 0.5 μg/ml; SI 42), the 2′,3′-dideoxythymidine derivative 3′-oximino-2′,3′-dideoxythymidine (EC501.5 μg/ml; SI 65), and 1-(2,3-dideoxy-3- N-hydroxyamino-β-d-threo-pentafuran yl)pentafuranosyl)thymine (EC50 4.1 μg/ml; SI >24).


2004 ◽  
Vol 15 (1) ◽  
pp. 3-15 ◽  
Author(s):  
Tatsuya Tsurumi ◽  
Masatoshi Fujita ◽  
Ayumi Kudoh

1993 ◽  
Vol 68 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Ichiro Honda ◽  
Harukuni Tokuda ◽  
Mutsuo Kozuka ◽  
Koichi Yoneyama ◽  
Hoyoku Nishino ◽  
...  

2003 ◽  
Vol 66 (12) ◽  
pp. 1582-1585 ◽  
Author(s):  
Kenji Iwatsuki ◽  
Toshihiro Akihisa ◽  
Harukuni Tokuda ◽  
Motohiko Ukiya ◽  
Manabu Oshikubo ◽  
...  

1988 ◽  
Vol 51 (6) ◽  
pp. 1266-1270 ◽  
Author(s):  
Takao Konoshima ◽  
Emiko Okamoto ◽  
Mutsuo Kozuka ◽  
Hoyoku Nishino ◽  
Harukuni Tokuda ◽  
...  

2000 ◽  
Vol 78 (1) ◽  
pp. 31-40 ◽  
Author(s):  
Hironori Ohtsu ◽  
Reiko Tanaka ◽  
Yasuko In ◽  
Shunyo Matsunaga ◽  
Harukuni Tokuda ◽  
...  

A new podocarpane diterpene, 7α,15-dihydroxypodocarp-8(14)-en-13-one (1) and eight new abietane diterpenes, abiet-8(14)-en-7α,13β,15,18-tetraol (2), 7α,13β,15-trihydroxyabiet-8(14)-en-18-oic acid (3), 13β,18-dihydroxyabiet-8(14)-en-7-one (4), 13β,15,18-trihydroxyabiet-8(14)-en-7-one (5), 7-oxo-13β-methoxyabiet-8(14)- en-18-oic acid (7), abiet-8(14)-en-7α,12α,13β,18-tetraol (8), 7α,12α,13β-trihydroxyabiet-8(14)-en-18-oic acid (9), and abiet-8(14)-en-7α,12α,13β,15,18-pentaol (10) were isolated from the CHCl3 extract of the cones of Larix kaempferi. Their structures were determined on the basis of chemical and spectral evidence. The inhibitory effects of compounds 1-4 and 7-9 on Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA), were examined for a primary screening for anti-tumor promotors. Key words: Larix kaempferi, Pinaceae, cones, abietane, EBV-EA.


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