標題: Diversity-Oriented Synthesis of Angular Bis-benzimidazole Derivatives under Microwave Irradiation
作者: Chen, Chih-Hau
Chien, Ming-Hsien
Kuo, Min-Liang
Chou, Cheng-Ting
Lai, Jin-Ji
Lin, Shu-Fen
Thummanagoti, Suman
Sun, Chung-Ming
應用化學系
Department of Applied Chemistry
公開日期: 1-Nov-2009
摘要: Pharmaceutically interesting, angular bis-benzimidazoles with three appendages have been synthesized successfully through a diversity-oriented approach with soluble support under microwave irradiation. Polymer immobilized o-phenylenediamine was selectively N-acylated with 2-chloro-3-nitrobenzoic acid in a primary aromatic amino moiety. The obtained amide was cyclized to benzimidazole in an acidic condition, and subsequently nucleophilic aromatic substitution with different amines was performed. Successive reduction, cyclization with various aldehydes and activated isothiocyanates yielded angular biheterocyclic benzimidazoles in good quantities. Reaction progress on polymer support was precisely monitored using the conventional proton NMR spectroscopy. Preliminary screening results showed some of these interesting compounds exhibited moderately to good inhibition against vascular endothelial growth factor receptor 3 (VEGFR-3), which is related to invasion and migration of cancer cells.
URI: http://dx.doi.org/10.1021/cc900084s
http://hdl.handle.net/11536/6507
ISSN: 1520-4766
DOI: 10.1021/cc900084s
期刊: JOURNAL OF COMBINATORIAL CHEMISTRY
Volume: 11
Issue: 6
起始頁: 1038
結束頁: 1046
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