Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia
Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia
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3-叠氮基-3-脱氧胸苷、3-叠氮基-2,3-二脱氧尿苷、3-叠氮基-2,3-二脱氧-的几种2,5-脱水类似物的合成和抗病毒活性
DOI：
10.1021/jm00128a034
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发表时间：
1989
影响因子：
7.3
通讯作者：
Prusoff,WH
中科院分区：
文献类型：
--
作者：
Lin,TS;Shen,ZY;August,EM;Brankovan,V;Yang,H;Ghazzouli,I;Prusoff,WH
3 ′-叠氮基-3 ′-脱氧胸苷（AZT）、3 ′-叠氮基-2 ′，3 ′-双脱氧尿苷（AZU）、3 ′-叠氮基-2 ′，3 ′-双脱氧-5-溴尿苷、3 ′-叠氮基-2 ′，3 ′-双脱氧-5-碘尿苷的几种2，5 ′-脱水类似物，3 ′-脱氧胸苷和5-甲基-2 ′-脱氧异胞苷的3 ′-叠氮衍生物已被合成，以评价其潜在的抗HIV活性（人类免疫缺陷病毒）剂。这些2，5 '-脱水衍生物，化合物13-17，表现出显著的抗HIV-1活性，IC 50值分别为0.56、4.95、26.5、27.1和48 µ。与母体化合物AZT和AZU相比，相应的2，5 '-脱水类似物，化合物13和14，活性稍低。AZT具有细胞毒性，其TCID 60为29 µ，而AZT的2，5 '-脱水衍生物化合物13的毒性则大大降低，其TCID 50值> 100 µ。5-甲基-2H-脱氧异胞苷的2，5 '-脱水类似物也显示出抗HIV-1活性，IC 60值为12 µ。还在细胞培养物中评价了这些化合物对Rauscher-鼠白血病病毒（R-MuLV）的作用。其中，AZT、3 '-叠氮基-2'，3 '-双脱氧-5-碘尿苷、3'-叠氮基-2 '，3'-双脱氧-5-溴尿苷和2，5 '-脱水-3'-叠氮基-3 '-脱氧胸苷（13）的活性最高，IC 50值分别为0.023、0.21、0.23和0.27 µ。齐多夫定（AZT，Zidovudine）首先由Horwitz等人2合成，后来由Lin和Prusoff修改了该方法。3 3 ′-叠氮基-2 ′，3 ′-双脱氧尿苷（2，AZU）首先由Lin 4合成，随后Schinazi等5报道AZU（CS-87）具有显著的抗HIV活性。Lin等人6和Hirsch提到了AZT的许多生物化学和临床研究。7据报道，AZT在治疗
Several 2, 5'-anhydro analogues of 3'-azido-3'-deoxythymidine (AZT), 3'-azido-2', 3'-dideoxyuridine (AZU), 3'-azido-2', 3'-dideoxy-5-bromouridine, 3'-azido-2', 3'-dideoxy-5-iodouridine, and 3'-deoxythymidine and the 3'-azido derivative of 5-methyl-2'-deoxyisocytidine have been synthesized for evaluation as potential anti-HIV (human immunodeficiency virus) agents. These 2, 5'-anhydroderivatives, compounds 13-17, demonstrated significant anti-HIV-1activity with IC50 values of 0.56, 4.95, 26.5, 27.1, and 48 µ, respectively. Compared to that of the parent compounds AZT and AZU, the respective 2, 5'-anhydro analogues, compounds 13 and 14, were somewhat less active. Whereas AZT was cytotoxic with a TCID60 of 29 µ, the toxicity of the 2, 5'-anhydro derivative of AZT, compound 13, was reduced considerably to a TCID50 value of> 100 µ. The 2, 5'-anhydro analogue of 5-methyl-2/-deoxyisocytidine also demonstrated anti-HIV-1activity with an IC60 value of 12 µ. These compounds were also evaluated against Rauscher-Murine leukemia virus (R-MuLV) in cell culture. Among them, AZT, 3'-azido-2', 3'-dideoxy-5-iodouridine, 3'-azido-2', 3'-dideoxy-5-bromouridine, and 2, 5'-anhydro-3'-azido-3'-deoxythymidine (13) were found to be most active, with IC50 values of 0.023, 0.21, 0.23, and 0.27 µ, respectively.3'-Azido-3'-deoxythymidine (AZT, Zidovudine) was first synthesized by Horwitz et al. 2 and later by a modification of this procedure by Lin and Prusoff. 3 3'-Azido-2', 3'-dideoxyuridine (2, AZU) was first synthesized by Lin4 and, subsequently, Schinazi et al. 5 reported that AZU (CS-87) possesses significant anti-HIV activity. References to many biochemical and clinical studies of AZT have been presented by Lin et al. 6 and Hirsch. 7 AZT has been reported to be of marked benefit in the
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Tuftsin：一种激素样四肽，具有抗菌和抗肿瘤活性。
影响因子：
6.1
作者：
Nishioka,K;Amoscato,AA;Babcock,GF
通讯作者：
Babcock,GF
吞噬作用刺激肽 tuftsin 在人多形核白细胞和单核细胞上的特异性结合位点。
DOI：
10.1016/0006-291x(78)91032-x
发表时间：
1978
影响因子：
3.1
作者：
Y. Stabinsky;P. Gottlieb;V. Zakuth;Z. Spirer;M. Fridkin
通讯作者：
M. Fridkin
Tuftsin 和其他蛋白质中类似序列的功能
影响因子：
5.2
作者：
S. Segal;E. Tzehoval;M. Feldman
通讯作者：
M. Feldman
采用高效液相色谱法分析四肽促尿素商业制剂中的污染物。
DOI：
10.1016/s0021-9673(00)81826-9
发表时间：
1981
期刊：
Journal of chromatography
影响因子：
--
作者：
Amoscato,AA;Babcock,GF;Nishioka,K
通讯作者：
Nishioka,K
放射性标记的促吞噬素与人中性粒细胞的相互作用。
DOI：
10.1016/0161-5890(78)90125-6
发表时间：
1978
期刊：
Immunochemistry
影响因子：
--
作者：
Raghavan M.G. Nair;Raghavan M.G. Nair;Bruce E Ponce;H. Fudenberg
通讯作者：
H. Fudenberg