8-氨基-6-甲基-2-β-D-呋喃核糖基-1,2,3,5,6,7-六氮杂并四苯（7-氮杂-TCN）以及相应的2'-脱氧和阿拉伯核苷类似物的合成与细胞毒性研究
Synthesis and cytotoxicity studies of 8-amino-6-methyl-2-beta-D-ribofuranosyl-1,2,3,5,6,7-hexaazaacenaphthyle ne (7-aza-TCN) and the corresponding 2'-deoxy- and arabinonucleoside analogues.
作者信息
Kawasaki A M, Wotring L L, Townsend L B
机构信息
Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109-1065.
出版信息
J Med Chem. 1990 Dec;33(12):3170-6. doi: 10.1021/jm00174a012.
The tricyclic nucleoside 8-amino-6-N-methyl-2-beta-D-ribofuranosyl-1,2,3,5,6, 7-hexaazaacenaphthylene was synthesized from 8-amino-6-N-methyl-4-(methylthio)-2-beta-D-ribofuranosyl-1,2,3,5,6, 7-hexaazaacenaphthylene. The 2'-deoxy analogue of 5, 8-amino-6-N-methyl-2-(2-deoxy-beta-D-ribofuranosyl)-1,2,3,5,6, 7-hexaazaacenaphthylene (11), and the arabino analogue of (5), 8-amino-6-N-methyl-2-beta-D-arabinofuranosyl-1,2,3,5,6, 7-hexaazaacenaphthylene (14) were synthesized from 5. Nucleosides 2,3,4,5,11, and 14 were evaluated for potential anticancer activity by measuring their ability to inhibit the growth of L1210 and H. Ep. 2 tumor cells in vitro.
三环核苷8-氨基-6-N-甲基-2-β-D-呋喃核糖基-1,2,3,5,6,7-六氮杂并四苯是由8-氨基-6-N-甲基-4-(甲硫基)-2-β-D-呋喃核糖基-1,2,3,5,6,7-六氮杂并四苯合成的。5,8-氨基-6-N-甲基-2-(2-脱氧-β-D-呋喃核糖基)-1,2,3,5,6,7-六氮杂并四苯（11）的2'-脱氧类似物以及（5）的阿拉伯糖类似物8-氨基-6-N-甲基-2-β-D-阿拉伯呋喃糖基-1,2,3,5,6,7-六氮杂并四苯（14）由5合成。通过测量核苷2、3、4、5、11和14在体外抑制L1210和H.Ep.2肿瘤细胞生长的能力来评估它们的潜在抗癌活性。
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