Soluble polymer supported divergent synthesis of tetracyclic benzene-fused pyrazino/diazepino indoles: An advanced synthetic approach to bioactive scaffolds

Po Tsung Lin, Deepak B. Salunke, Li Hsun Chen, Chung-Ming Sun*

*Corresponding author for this work

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

The synthesis of indoline substituted nitrobenzene on a PEG support and its further elaboration to structurally diverse benzene-fused pyrazino/diazepino indoles is disclosed. A reagent based diversification approach coupled with Pictet-Spengler type condensation reactions furnished these fused polycyclic scaffolds. Microwave irradiation was used as a means of rate acceleration for soluble polymer-supported reactions. The efficiency of these fused heterocyclic molecules to inhibit the vascular endothelial growth factor receptor 3 (VEGFR-3) was examined in vitro using kinase receptor activation enzyme-linked immunosorbant assay (KIRA-ELISA). Based on the preliminary results obtained, a small set of potential drug candidates were identified as novel leads in this therapeutic area to be further explored as anti-metastatic agents.

Original languageEnglish
Pages (from-to)2925-2937
Number of pages13
JournalOrganic and Biomolecular Chemistry
Volume9
Issue number8
DOIs
StatePublished - 21 Apr 2011

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