2-Substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity
摘要:
1-Amino-3-(aminooxy)-2-propanol (6a) has been synthesized and found to inhibit rat liver ornithine decarboxylase (ODC) with an IC50 in the nanomolar range. Compound 6a served as a basis for the design of new enzyme inhibitors, which led to the identification of 3-(aminooxy)-2-fluoropropanamine (15) as a new powerful enzyme blocker. Compound 15 inhibited ODC at 3 times lower concentrations than 6a and 3-(aminooxy)propanamine (APA), and it was superior to APA as an antiproliferative agent in inhibiting the growth of human T24 bladder carcinoma cells in vitro.
2-Substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity
摘要:
1-Amino-3-(aminooxy)-2-propanol (6a) has been synthesized and found to inhibit rat liver ornithine decarboxylase (ODC) with an IC50 in the nanomolar range. Compound 6a served as a basis for the design of new enzyme inhibitors, which led to the identification of 3-(aminooxy)-2-fluoropropanamine (15) as a new powerful enzyme blocker. Compound 15 inhibited ODC at 3 times lower concentrations than 6a and 3-(aminooxy)propanamine (APA), and it was superior to APA as an antiproliferative agent in inhibiting the growth of human T24 bladder carcinoma cells in vitro.
Method for utilizing triethylaluminum to prepare an alumoxane support for an active metallocene catalyst
申请人:EXXON CHEMICAL PATENTS INC.
公开号:EP0368644A1
公开(公告)日:1990-05-16
This invention relates to a process for preparing a supported metallocene alumoxane catalyst for use in the polymerization of olefins. The invention particularly relates to the use of silica gel containing from about 6 to about 20 per cent by weight adsorbed water as the catalyst support material. It has been found that such silica gel may be safely added to a solution, of trialkylaluminum to form by direct reaction with the adsorbed water content of the silica gel catalyst support material the majority of the alumoxane component requirement of the catalyst system. An alkylalumoxane coated silica gel is formed to which a trimethylaluminum treated metallocene may be added and the resulting material dried to free-flowing powder. The dry free flowing powder may then be used as a supported metallocene alumoxane catalyst complex for gas phase or liquid phase polymerization of olefins. The supported catalyst produced by such procedure has an activity at least comparable to a catalyst of similar composition which is produced exclusively with trimethylaluminum as the alumoxane forming aluminum alkyl.
Verbindungen der Formel I
worin R₁, R₂, R₃ und X die in der Beschreibung angegebenen Bedeutungen haben, weisen wertvolle pharmazeutische Eigenschaften auf und sind insbesondere gegen Tumoren wirksam. Sie werden in an sich bekannter Weise hergestellt.
式 I 的化合物
其中 R₁、R₂、R₃ 和 X 的含义在描述中给出。它们以已知的方式生产。
2-Substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity
1-Amino-3-(aminooxy)-2-propanol (6a) has been synthesized and found to inhibit rat liver ornithine decarboxylase (ODC) with an IC50 in the nanomolar range. Compound 6a served as a basis for the design of new enzyme inhibitors, which led to the identification of 3-(aminooxy)-2-fluoropropanamine (15) as a new powerful enzyme blocker. Compound 15 inhibited ODC at 3 times lower concentrations than 6a and 3-(aminooxy)propanamine (APA), and it was superior to APA as an antiproliferative agent in inhibiting the growth of human T24 bladder carcinoma cells in vitro.