Chiang Chi-Shiun, Yu Ching-Fang, Chiang Li-Wu, Chen Shao-Wei, Lo Jem-Mau, Yu Chung-Shan
Department of Biomedical Engineering and Environmental Sciences, National Tsing-Hua University, Hsinchu, Taiwan.
Chem Pharm Bull (Tokyo). 2008 Jan;56(1):109-11. doi: 10.1248/cpb.56.109.
A cell survival assay of the four arabinosyl uridine analogs with functionalities of 5-fluoro, 5-fluorovinyl, 5-iodo, and 5-iodovinyl as potential positron-emitter tagged probe for monitoring cancer gene therapy were performed. Cytotoxicities of 5-fluoro-, 5-iodo-, 5-fluorovinyl, and 5-iodovinyl arabinosyl uridines against SR-39 thymidine kinase transfected murine prostate cancer cells have been evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. None of them showed significant bioactivity. A syn conformation derived from intra-hydrogen bonding was suggested for the unfavorable interaction and diminished bioactivity.
进行了四种具有5-氟、5-氟乙烯基、5-碘和5-碘乙烯基官能团的阿拉伯糖基尿苷类似物作为监测癌症基因治疗的潜在正电子发射体标记探针的细胞存活试验。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐试验评估了5-氟-、5-碘-、5-氟乙烯基和5-碘乙烯基阿拉伯糖基尿苷对SR-39胸苷激酶转染的小鼠前列腺癌细胞的细胞毒性。它们均未显示出显著的生物活性。对于不利的相互作用和生物活性降低，提出了一种由分子内氢键产生的顺式构象。
