BORONIC ACID ANALOGS OF NUCLEOSIDE-5'-PHOSPHATES

5-磷酸核苷硼酸类似物

基本信息

  • 批准号:
    3498936
  • 负责人:
  • 金额:
    $ 5万
  • 依托单位:
  • 依托单位国家:
    美国
  • 项目类别:
  • 财政年份:
    1993
  • 资助国家:
    美国
  • 起止时间:
    1993-02-01 至 1993-11-30
  • 项目状态:
    已结题

项目摘要

A major problem with the use of nucleoside phosphates as antiviral and antitumor drugs has been their inability to penetrate cell membranes. Additionally, nucleoside phosphates are susceptible to phosphatases and nucleases, which reduce their in vivo life time. Replacement of the charged phosphate group with uncharged boron containing moieties should not only enhance their cell permeability, but the new analogs are expected to be resistant to phosphatases and nucleases. The long term objective of this project is to synthesize boronated nucleoside phosphates as analogs of normal or sugar modified nucleosides. These compounds may be prepared by two methods: 1) by direct modification of a nucleoside or 2) by attachment of a modified sugar moiety to the base. The Phase I effort will mainly concentrate on the synthesis of an analog of acyclovir monophosphate and to develop methods that may be utilized for the synthesis of analogs of other nucleoside phosphates in Phase II. The newly synthesized compound will be tested for its effect on certain enzymes and its potential antitumor and antiviral activity. The boronated nucleotides may be useful in a number of ways including: 1) as tools for studying mechanism of action of enzymes 2) as antiviral and antitumor agents, and 3) as carriers of boron-10 for boron neutron capture therapy.
使用磷酸核苷作为抗病毒药物的一个主要问题

项目成果

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BERNARD F SPIELVOGEL其他文献

BERNARD F SPIELVOGEL的其他文献

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{{ truncateString('BERNARD F SPIELVOGEL', 18)}}的其他基金

NEW (B22H22)2 FOR NEUTRON CAPTURE AND DIAGNOSTICS
用于中子捕获和诊断的新型 (B22H22)2
  • 批准号:
    2776444
  • 财政年份:
    1999
  • 资助金额:
    $ 5万
  • 项目类别:
SELECTIVE SILVER STAINING OF DNA PROBES
DNA 探针的选择性银染
  • 批准号:
    2191916
  • 财政年份:
    1995
  • 资助金额:
    $ 5万
  • 项目类别:
REPRODUCTIVE TOXICOLOGY OF BORON ANALOGS OF BIOMOLECULES
生物分子硼类似物的生殖毒理学
  • 批准号:
    2203890
  • 财政年份:
    1994
  • 资助金额:
    $ 5万
  • 项目类别:
BORONATED ASPARAGINE AND GLUTAMINE ANALOGS FOR BNCT
BNCT 的硼化天冬酰胺和谷氨酰胺类似物
  • 批准号:
    2108414
  • 财政年份:
    1994
  • 资助金额:
    $ 5万
  • 项目类别:
AMINE-BORANES AS NEW TOPOISOMERASE II INHIBITORS
胺硼烷作为新的拓扑异构酶 II 抑制剂
  • 批准号:
    3493267
  • 财政年份:
    1993
  • 资助金额:
    $ 5万
  • 项目类别:
BORONATED NUCLEOSIDE BASES
硼化核苷碱基
  • 批准号:
    3493427
  • 财政年份:
    1993
  • 资助金额:
    $ 5万
  • 项目类别:
NUCLEOSIDE PHOSPHATE ANALOGUES WITH BORONATED PHOSPHATES
含硼磷酸盐的核苷磷酸类似物
  • 批准号:
    3489416
  • 财政年份:
    1991
  • 资助金额:
    $ 5万
  • 项目类别:
NUCLEOSIDE PHOSPHATE ANALOGS WITH BORONATED PHOSPHATES
含硼磷酸盐的核苷磷酸类似物
  • 批准号:
    2065963
  • 财政年份:
    1991
  • 资助金额:
    $ 5万
  • 项目类别:
OLIGONUCLEOTIDES WITH BORONATED PHOSPHORUS BACKBONES
具有硼化磷骨架的寡核苷酸
  • 批准号:
    3506903
  • 财政年份:
    1991
  • 资助金额:
    $ 5万
  • 项目类别:
NUCLEOSIDE PHOSPHATE ANALOGS WITH BORONATED PHOSPHATES
含硼磷酸盐的核苷磷酸类似物
  • 批准号:
    2065962
  • 财政年份:
    1991
  • 资助金额:
    $ 5万
  • 项目类别:

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