Comparison of bioactivities of 5-Fluoro, 5-Iodo, 5-Iodovinyl, and 5-fluorovinyl arabinosyl uridines against SR-39 TK-transfected murine prostate cancer cells.
نویسندگان
چکیده
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.
منابع مشابه
Synthesis and Enzymatic Evaluation of Nucleosides Derived from 5-Iodo-2’-Halo-2’-Deoxyuridines
The synthesis of new nucleosides by alkenylation of 5-iodo-2’-halo-2’-deoxyuridines with E-(1-tributylstannyl)-propene-1-ol via STILLE-coupling is described. The new compounds are characterized by 1H NMR and elemental analysis. All nucleosides are evaluated by an enzymatic assay to be substrates of herpes simplex virus type 1 thymidine kinase (HSV-1 TK) and compared with uridine, thymidine and ...
متن کاملThe lethality of some D-arabinosyl nucleotides to mouse fibroblasts.
1This study was supported by American Cancer Society Grant E587. 'Present address: University of Pennsylvania, School of Veterinary Medicine, New Bolton Center, Kennen Square, Pa. 19348. 3To whom reprint requests should be addressed. Present address: University of Colorado Medical Center, Department of Microbiology, Denver, Colo. 80220. 4The abbreviations used are: FdUrd, 5-fluoro-2-deoxyuridin...
متن کاملImaging the expression of transfected genes in vivo.
Imaging the expression of successful gene transduction has been demonstrated in vivo for the first time by using an appropriate combination of "marker gene" and "marker substrate" in an experimental animal model. The herpes simplex virus 1 thymidine kinase (HSV1-tk) gene was selected as an example of a marker gene, and the recombinant STK retrovirus containing HSV1-tk was used to transduce RG2 ...
متن کاملThe Lethality of Some D-Arabinosyl Nucleotides to Mouse Fibroblasts1
1This study was supported by American Cancer Society Grant E587. 'Present address: University of Pennsylvania, School of Veterinary Medicine, New Bolton Center, Kennen Square, Pa. 19348. 3To whom reprint requests should be addressed. Present address: University of Colorado Medical Center, Department of Microbiology, Denver, Colo. 80220. 4The abbreviations used are: FdUrd, 5-fluoro-2-deoxyuridin...
متن کاملSynthesis of homologated halovinyl derivatives from aristeromycin and their inhibition of human placental S-adenosyl-L-homocysteine hydrolase.
Moffatt oxidation of 2',3'-O-isopropylidenearisteromycin (1a) and treatment of the 5'-carboxaldehyde with [(p-tolylsulfonyl)methylene]triphenylphosphorane gave the homologated vinylsulfone 2. Treatment of 2 with tributylstannane/AIBN gave the (E/Z)-vinylstannanes which were converted into the E and Z fluoro- and iodovinyl analogs. Chain extension via the 5'-cyano-5'-deoxy derivative 10a gave th...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Chemical & pharmaceutical bulletin
دوره 56 1 شماره
صفحات -
تاریخ انتشار 2008