发明名称 Heterocyclic amine-boranes, and method of inhibiting DNA topoisomerase activity and/or combatting inflammation, hyperlipidemia, and/or neoplasia using amine-borane compounds
摘要 Heterocyclic amine-borane compounds of formula (I) wherein: A is a heterocyclic amine moiety; R1 is selected from H, alkyl, alkylaryl, aryl, and arylalkyl; and R2 is selected from CN, COOH, COOR3, and CONHR3 where R3 is selected from H, alkyl, alkylaryl, aryl, aralkyl. The heterocyclic amine-borane compounds of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and anti-hyperlipidemic activity. The invention also comprehends a method of inhibiting enzyme activity (e.g., DNA topoisomerase II, PRPP amidotransferase, IMP dehydrogenase, dihydrofolate reductase, and/or ribonucleotide reductase) in an in vitro or in vivo system, comprising administering to the system an enzyme-inhibitingly effective amount of a Lewis-base borane adduct, such as a heterocyclic amine-borane compound of the foregoing formula.
申请公布号 US5280119(A) 申请公布日期 1994.01.18
申请号 US19910786279 申请日期 1991.11.01
申请人 BORON BIOLOGICALS, INC. 发明人 SPIELVOGEL, BERNARD F.;SOOD, ANUP;HALL, IRIS H.
分类号 C07F5/02;(IPC1-7):C07F5/02;A61K33/22;A61K43/00 主分类号 C07F5/02
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