Comparison of bioactivities of 5-Fluoro, 5-Iodo, 5-Iodovinyl, and 5-fluorovinyl arabinosyl uridines against SR-39 TK-transfected murine prostate cancer cells.
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.
Chiang
Chi-Shiun
CS
Department of Biomedical Engineering and Environmental Sciences, National Tsing-Hua University, Hsinchu, Taiwan.
Yu
Ching-Fang
CF
Chiang
Li-Wu
LW
Chen
Shao-Wei
SW
Lo
Jem-Mau
JM
Yu
Chung-Shan
CS
D000818:Animals; D004354:Drug Screening Assays, Antitumor; D015316:Genetic Therapy / Q000379:methods; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011471:Prostatic Neoplasms; D013329:Structure-Activity Relationship; D013937:Thymidine Kinase / Q000235:genetics* / Q000378:metabolism; D014529:Uridine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
C525774:5-fluoro arabinosyl uridine; C525777:5-fluorovinyl arabinosyl uridine; C525775:5-iodo arabinosyl uridine; C525776:5-iodovinyl arabinosyl uridine; D013937:Thymidine Kinase; D014529:Uridine