Efficient Synthetic Protocol and Mechanistic Study of Quinazoline Analogues and their Biological Importance

Abstract

Our main focus is on the recent developments for the synthesis of highly functionalized quinazoline derivatives in terms of an efficient, one-pot, eco-friendly, solvent-free, high yield, cost-effective, multicomponent strategy with the variation of substrates and catalytic conditions. Further, we have also emphasized on the mechanistic studies depending upon variation of substrates. Detailed mechanistic aspects have been established based on isolated intermediates and their single crystal X-ray structures. The biological importance of selected small quinazoline derivatives has been highlighted as well. In particular, we have observed that selected quinazolinebased small molecules show global upregulation of miRNA expression with a selective enrichment of tumor suppressor miRNAs. Therefore, quinazolines can be used as scaffolds to design activator of miRNA expression, thus paving the way for the development of novel anti-cancer drugs.

Keywords: Anti-cancer drug, Biological activity, Global upregulation of miRNA, miRNA upregulation, Multicomponent one-pot synthetic protocol, Nitrogen heterocycle molecules, Quinazoline synthesis.

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