標題: Polymer supported synthesis of novel benzoxazole linked benzimidazoles under microwave conditions: In vitro evaluation of VEGFR-3 kinase inhibition activity
作者: Chanda, Kaushik
Maiti, Barnali
Yellol, Gorakh S.
Chien, Ming-Hsien
Kuo, Min-Liang
Sun, Chung-Ming
應用化學系
Department of Applied Chemistry
公開日期: 2011
摘要: An efficient soluble polymer-supported method has been developed for the parallel synthesis of substituted benzimidazole linked benzoxazoles using focused microwave irradiation. The key step involves the amidation of 4-hydroxy-3-nitrobenzoic acid with polymer-immobilized o-phenylenediamine. Application of mild acidic conditions promoted the ring closure to furnish the benzimidazole ring. After hydrogenation of the nitro-group to amine, the resulted polymer conjugates underwent efficient ring closure with various alkyl, aryl and heteroaryl isothiocyanates to generate the polymer-bound benzimidazolyl benzoxazoles. The polymer-bound compounds were finally cleaved from the support to furnish benzimidazole linked benzoxazole derivatives. The efficacy of the resultant angular bis-heterocyclic library was studied against vascular endothelial growth factor receptor (VEGFR-3). The preliminary screening of these novel compounds exhibits moderate to high inhibition (IC(50) = 0.56-1.42 mM). This protocol provides an easy access to novel angular bis-heterocycles which have potential for the discovery of novel leads for targeted cancer therapeutics.
URI: http://hdl.handle.net/11536/26041
http://dx.doi.org/10.1039/c0ob00547a
ISSN: 1477-0520
DOI: 10.1039/c0ob00547a
期刊: ORGANIC & BIOMOLECULAR CHEMISTRY
Volume: 9
Issue: 6
起始頁: 1917
結束頁: 1926
Appears in Collections:Articles


Files in This Item:

  1. 000287931500032.pdf