Balzarini J, Bernaerts R, Verbruggen A, De Clercq E
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
Mol Pharmacol. 1990 Mar;37(3):402-7.
The carbocyclic analogue of (E)-5-(2-iodovinyl)-2'-deoxyuridine (C-IVDU) is, like its parent compound (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU), a potent and selective inhibitor of herpes simplex virus type 1 (HSV-1). There is a close correlation between the inhibition of viral DNA synthesis and the antiviral activity of both IVDU and C-IVDU. IVDU and C-IVDU inhibit viral DNA synthesis at 0.2 and 0.5 microM, respectively, and interfere with cellular DNA synthesis at concentrations that are 10- to 40-fold in excess of their antivirally effective doses. At concentrations affording a similar antiviral effect, C-[125I]IVDU is incorporated into viral and cellular DNA of HSV-1-infected Vero cells to a 7- to 10-fold lesser extent than IVDU. [125I]IVDU but not C-[125I]IVDU leads to breakage of both DNA strands when incorporated into HSV-1 DNA.
（E）-5-（2-碘乙烯基）-2'-脱氧尿苷（C-IVDU）的碳环类似物与其母体化合物（E）-5-（2-碘乙烯基）-2'-脱氧尿苷（IVDU）一样，是1型单纯疱疹病毒（HSV-1）的强效和选择性抑制剂。病毒DNA合成的抑制与IVDU和C-IVDU的抗病毒活性之间存在密切相关性。IVDU和C-IVDU分别在0.2和0.5微摩尔浓度下抑制病毒DNA合成，并在超过其抗病毒有效剂量10至40倍的浓度下干扰细胞DNA合成。在提供相似抗病毒效果的浓度下，C-[125I]IVDU掺入HSV-1感染的Vero细胞的病毒和细胞DNA中的程度比IVDU低7至10倍。[125I]IVDU而非C-[125I]IVDU掺入HSV-1 DNA时会导致两条DNA链断裂。
