Synthesis and Biochemical Activity of Hydrophilic Carborane-Containing Pyrimidine Nucleosides as Potential Agents for DNA Incorporation and BNCT |
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| Authors: | Feng-Guang Rong Albert H. Soloway Seiichiro Ikeda David H. Ives |
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| Affiliation: | 1. College of Pharmacy, The Ohio State University , 500 West 12th Avenue, Columbus, OH, 43210, U.S.A.;2. College of Biological Sciences, The Ohio State University , 500 West 12th Avenue, Columbus, OH, 43210, U.S.A. |
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| Abstract: | Abstract A novel type of hydrophilic 5-tethered carborane-containing 2′-deoxyuridine derivative, SUB-7-DIOL, has been developed. This compound is a potential agent for DNA incorporation and BNCT, because it showed satisfactory aqueous solubility and demonstrated an excellent rate of phosphorylation by human thymidine kinase. This study also demonstrated the importance of tethering a flexible hydrocarbon chain between the carborane cage and the 5-position of the nucleoside, and the effectiveness of a water-solubilizing moiety attached to the carbon atom of the lipophilic carborane cage. |
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| Keywords: | Thieno[2,3-d]pyrimidines cyclic and acyclic nucleosides antimicrobial activity |
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