Fedorov I I, Kraevskiĭ A A, Bal'zarinin Zh, De Klerk E
Mol Biol (Mosk). 1992 Sep-Oct;26(5):1122-7.
Inhibition of HIV-1- or HIV-2-induced cytopathicity and (Moloney) murine sarcoma virus (MSV)-induced cell transformation by amino acid and amino alcohol adducts of either 3'-azido-2',3'-dideoxythymidine 5'-monophosphate (AZTMP) or 5'-hydrogenphosphonate (AZTHP) were investigated. Both types of nucleotide adducts inhibited replication of HIV-1 and HIV-2 in MT-4 cells at a 1.5- to 3-fold higher EC50 (50% effective concentration) than AZT; and, also, selectivity indexes of these adducts were approximately 1.5 to 3-fold lower than that of AZT. The activity of the AZTMP and AZTHP adducts against MSV-induced transformation of C3H/3T3 cells was equal to or only slightly inferior than that of AZT, but their toxicity was 10-fold lower, so that their selectivity indexes were 2- to 7-fold higher. The nature of the aminoacyl component of the adducts significantly influence the antiretroviral activity of the test compounds.
研究了3'-叠氮-2',3'-二脱氧胸苷5'-单磷酸（AZTMP）或5'-氢膦酸酯（AZTHP）的氨基酸和氨基醇加合物对HIV-1或HIV-2诱导的细胞病变以及（莫洛尼）鼠肉瘤病毒（MSV）诱导的细胞转化的抑制作用。两种类型的核苷酸加合物在MT-4细胞中抑制HIV-1和HIV-2复制的半数有效浓度（EC50）比齐多夫定（AZT）高1.5至3倍；而且，这些加合物的选择性指数比AZT低约1.5至3倍。AZTMP和AZTHP加合物对MSV诱导的C3H/3T3细胞转化的活性与AZT相当或仅略低于AZT，但其毒性低10倍，因此它们的选择性指数高2至7倍。加合物的氨酰基成分的性质显著影响受试化合物的抗逆转录病毒活性。
