AMINE-BORANES AS NEW TOPOISOMERASE II INHIBITORS
AMINE-BORANES AS NEW TOPOISOMERASE II INHIBITORS
批准号:
3493267
负责人:
BERNARD F SPIELVOGEL
金额:
$5.0万
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
项目状态:
已结题
起止时间:
1993-05-01 至 1993-10-31
中文摘要
本研究的主要目的是开发一类新型的
英文摘要
The main objective of the proposed research is to develop a new class of
topoisomerase II (Topo II) inhibitors as antineoplastic agents. In
preliminary studies, heterocyclic amine-carboxyboranes have been shown to
possess cytotoxic activity against a number of murine and human tumor
tissue culture lines, e.g. P388, L1210, Tmolt3, HeLa-S3, lung
brochogenic, KB nasopharynx, glioma, and osteosarcoma. These compounds
have been shown to inhibit HeLa-S3 Topo II at 100 mu M concentration, but
have not been tested below this concentration.
The phase I objectives are to synthesize a larger selection of
amine-carboxyboranes to evaluate the effect of Lewis base moiety on
biological activity. Studies are proposed to determine in vitro
cytotoxicity and in vivo antitumor activity of these compounds. Mode of
action studies will be limited to Topo II inhibition, inhibition of DNA
synthesis and DNA stability in phase I.
Phase II studies will concentrate further on structure-activity
relationship with the help of molecular modeling. In addition, detailed
mode of action, acute toxicity, tissue disposition, and pharmacokinetic
parameters will be determined.
The proposed project is expected to result in the identification and
development of one or more potent antineoplastic agents to treat one or
more human tumors.
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会议论文
NEW (B22H22)2 FOR NEUTRON CAPTURE AND DIAGNOSTICS
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批准号:2776444
-
项目类别:
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资助金额:$10.0万
-
财政年份:1999
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
SELECTIVE SILVER STAINING OF DNA PROBES
-
批准号:2191916
-
项目类别:
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资助金额:$10.0万
-
财政年份:1995
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
REPRODUCTIVE TOXICOLOGY OF BORON ANALOGS OF BIOMOLECULES
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批准号:2203890
-
项目类别:
-
资助金额:$7.3万
-
财政年份:1994
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
BORONATED ASPARAGINE AND GLUTAMINE ANALOGS FOR BNCT
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批准号:2108414
-
项目类别:
-
资助金额:$7.94万
-
财政年份:1994
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
BORONATED NUCLEOSIDE BASES
-
批准号:3493427
-
项目类别:
-
资助金额:$5.0万
-
财政年份:1993
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
BORONIC ACID ANALOGS OF NUCLEOSIDE-5'-PHOSPHATES
-
批准号:3498936
-
项目类别:
-
资助金额:$5.0万
-
财政年份:1993
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
NUCLEOSIDE PHOSPHATE ANALOGUES WITH BORONATED PHOSPHATES
-
批准号:3489416
-
项目类别:
-
资助金额:$4.99万
-
财政年份:1991
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
NUCLEOSIDE PHOSPHATE ANALOGS WITH BORONATED PHOSPHATES
-
批准号:2065963
-
项目类别:
-
资助金额:$24.62万
-
财政年份:1991
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
OLIGONUCLEOTIDES WITH BORONATED PHOSPHORUS BACKBONES
-
批准号:3506903
-
项目类别:
-
资助金额:$25.01万
-
财政年份:1991
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
NUCLEOSIDE PHOSPHATE ANALOGS WITH BORONATED PHOSPHATES
-
批准号:2065962
-
项目类别:
-
资助金额:$24.91万
-
财政年份:1991
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
OLIGONUCLEOTIDES WITH BORONATED PHOSPHORUS BACKBONES
-
批准号:3506904
-
项目类别:
-
资助金额:$24.86万
-
财政年份:1991
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
OLIGONUCLEOTIDES WITH BORONATED PHOSPHORUS BACKBONES
-
批准号:3498192
-
项目类别:
-
资助金额:$5.0万
-
财政年份:1988
-
负责人:BERNARD F SPIELVOGEL
-
依托单位:
海外基金