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ChemInform Abstract: Synthesis and Biological Activity of Aromatic Amino Acid Phosphoramidates of 5-Fluoro-2′-deoxyuridine and 1-β- Arabinofuranosylcytosine: Evidence of Phosphoramidase Activity.

✍ Scribed by T. W. ABRAHAM; T. I. KALMAN; E. J. MCINTEE; C. R. WAGNER

Book ID
101845455
Publisher
John Wiley and Sons
Year
2010
Weight
35 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

Synthesis and Biological Activity of Aromatic Amino Acid Phosphoramidates of 5-Fluoro-2'-deoxyuridine and 1-β-Arabinofuranosylcytosine: Evidence of Phosphoramidase Activity.

-The title compounds (IV) and (VII) are tested for their antitumor activity against L1210 mouse lymphocytic leukemia cells and CCRF-CEM human T-cells lymphoblastic leukemia cells. The compounds (VII) are found to be inactive at a concentration of 100 µM, while the derivatives (IV) exhibit IC50 values within a range of 0.30-0.40 µM. Furthermore, mechanistic studies conducted to determine the extra-and intracellular behavior of these compounds are described.

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ChemInform Abstract: Synthesis and Biolo
ChemInform Abstract: Synthesis and Biological Activity of Bis(pivaloyloxymethyl) Ester of 2′-Azido-2′-deoxyuridine 5′-Monophosphate.
✍ S. H. KANG; A. K. SINHABABU; M. J. CHO 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 28 KB 👁 1 views

Synthesis and Biological Activity of Bis(pivaloyloxymethyl) Ester of 2'-Azido-2'-deoxyuridine 5'-Monophosphate. -The title compound (III) which is the membrane-permeable prodrug of the phosphate (I), is evaluated with positive results for inhibition of cell growth with 60 tumor cell lines.