16401-93-7

Upstream product

• 123-76-2 levulinic acid 
• 19501-58-7 4-methoxyphenylhydrazine hydrochloride 
• 586-75-4 4-chlorobenzoyl chloride 
• 3471-32-7 4-Methoxyphenylhydrazine 
• 13815-71-9 1-ethylidene-2-(4-methoxyphenyl)hydrazine 
• 345960-79-4 acetaldehyde N₁-(4-bromobenzoyl)-N₁-(4-methoxyphenyl)hydrazone 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of an Indomethacin Library Reveals a New Class of Angiogenesis-Related Kinase Inhibitors

Capture and release: Indomethacin has served as a lead compound for the synthesis of a library that revealed a new class of kinase inhibitors. A synthetic approach termed "resin-capture-release" was developed (see scheme) that allowed a large library to be synthesized easily. Six of the library compounds were found to be inhibitors of angiogenesis-related receptor tyrosine kinases.

Modulation of MRP-1-mediated multidrug resistance by indomethacin analogues

Multidrug resistance (MDR) is a major limiting factor in the development and application of drug candidates. MDR caused by MRP-1 is known to be modulated by the nonsteroidal antiinflammatory drug indomethacin. We have synthesized and biologically evaluated a library of indomethacin analogues. The indomethacin-derived compound library was synthesized employing the Fischer-indole synthesis as the key transformation and making use of a resin-capture-release strategy. Sixty representative members of the library were evaluated in a cell biological cytotoxicity assay employing the MRP-1 expressing human glioblastoma cell line T98G as a model system. Nine of the 60 tested derivatives increased the doxorubicin-mediated cytotoxicity at a comparable or higher level than indomethacin itself. Analysis of these derivatives revealed an interesting structure-function relationship. Most remarkably, two substances increased the toxicity, when doxorubicin was used at clinically relevant low concentrations, at a higher degree than indomethacin.

Synthesis of indomethacin analogues for evaluation as modulators of MRP activity

Synthesis of a range of indomethacin analogues, required for investigation in combination toxicity assays, bearing both N-benzyl and N-benzoyl groups, is described. Copyright