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Acridone derivatives are selective inhibitors of HIV-1 replication in chronically infected cells.
The results suggest that the acridone derivatives suppress HIV-1 replication at the transcriptional level primarily through a mechanism of PKC inhibition.
Endothelium-derived hyperpolarizing factor does not contribute to the decrease in endothelium-dependent relaxation in the aorta of streptozotocin-induced diabetic rats.
While endothelium-derived NO appears to contribute to the impairment of ACh-induced endothelia-dependent relaxation in the aorta of diabetic rats, EDHF does not, and N omega-L-nitro-arginine methylester and tetraethylammonium chloride (TEA) is used to inhibit nitric oxide and EDHF.
Synthesis and antiherpesviral activity of 5-C-substituted uracil nucleosides.
Reaction of 2'-deoxy-5-hydroxyuridine with some Wittig reagents gave 5-alkoxycarbonylmethyl-, 5-carbamoylmethyl, 5-cyanomethyl- and 5-acetonyl-2'-dexyuridines, which showed marked antiherpesviral activity in vitro.
Deglycosylation of antiherpesviral 5-substituted arabinosyluracil derivatives by rat liver extract and enterobacteria cells.
It is suggested that antiherpesviral 5-substituted araU analogues can be relatively stable in vivo, when injected intravenously, and that degradation of 1-beta-D-arabinofuranosyl-5-(E-2-bromovinyl)uracil (sorivudine) following oral administration is due primarily to the action of enterobacteria.
Comparison of 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine with gemcitabine in its antitumor activity.
4'-thio-FAC inhibited tumor growth more strongly than gemcitabine did at the same dose against human cancer cells implanted s.c. in nude mice, and suppressed the tumor growth by oral administration.
Differential activity of potential antiviral nucleoside analogs on herpes simplex virus-induced and human cellular thymidine kinases
The amount of the analogs phosphorylated to the monophosphate form, which is presumably necessary to produce cytotoxic effects, was determined by the combined effects of phosphorylation rates and binding affinities.
Comparison of two bromovinyl nucleoside analogs, 1-beta-D-arabinofuranosyl-E-5-(2-bromovinyl)uracil and E-5-(2-bromovinyl)-2'-deoxyuridine, with acyclovir in inhibition of Epstein-Barr virus
  • J. Lin, H. Machida
  • Biology, Medicine
    Antimicrobial Agents and Chemotherapy
  • 1 July 1988
Kinetic analysis of reversibility of inhibition of EBV DNA replication after removal of the drugs indicated that BV-araU, like BVdU, has a more prolonged inhibitory effect than ACV.
Comparison of susceptibilities of varicella-zoster virus and herpes simplex viruses to nucleoside analogs
  • H. Machida
  • Medicine, Biology
    Antimicrobial Agents and Chemotherapy
  • 1 March 1986
Against VZV the 5-halogenovinyl-arabinosyluracils were the most potent of the compounds tested and were different from that of HSV-1.
Antitumor activity of a novel orally effective nucleoside, 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine.
4'-Thio-FAC showed a remarkable antitumor effect against human tumors subcutaneously implanted into nude mice and was highly effective even by oral administration, and therefore is a promising drug candidate for cancer chemotherapy.
Differential vasodilatory action of 2-octynyladenosine (YT-146), an adenosine A2 receptor agonist, in the isolated rat femoral artery and vein.
The present study did not provide evidence of a link between adenosine agonist-induced vasodilation andAdenosine A2 receptor activation in the artery, and the vasodilatory action of N6-cyclopentyladenosine (CPA) was much weaker in the vein than that of YT-146.