Abstract
A library of 4H-chromene derivatives with heterocyclic substituent's at the 3 and 4-positions was synthesized in a convenient DBU catalysed three component synthesis between salicylaldehyde, acetonitrile derivatives and thiazolidinedione to afford 2-amino-3-benzothiazole-4-heterocycle-4H-chromenes and 2-amino-3-thiophenoyl-4-heterocycle-4H-chromenes derivatives in ethanol and a mixture of ethanol and water (1 : 1) at room temperature. The significance of this protocol is the feasibility of incorporating substituents simultaneously at the 3 and 4 positions of 4H-chromenes in an efficient three component reaction.
Highlights
The design of highly functionalized small organic molecules with features suited for highly selective binding to macromolecules is crucial to accelerate the drug discovery process.[1]
; the synthesis of molecules that are enriched with therapeutic values has become the main objective for organic and medicinal chemistry research projects
As a result the model reaction was performed between heterocyclic carbon nucleophile (1.0 equiv.) (1a), salicylaldehyde (1.0 equiv.) (2a), and benzothiazole acetonitrile (1.2 equiv.) (3) at room temperature to afford the required product in 95% yield in 2 h (Scheme 2)
Summary
The design of highly functionalized small organic molecules with features suited for highly selective binding to macromolecules is crucial to accelerate the drug discovery process.[1]. The anticancer activity of these molecules may be attributed to the formation of reactive intermediates that can bind covalently to DNA.[21] Modi cations on the benzothiazole nucleus have resulted in a large number of hybrids having diverse pharmacological activities. The excellent antitumour potential of these hybrid molecules have attracted our attention to synthesize heterocyclic hybrids of benzothiazole and 4substituted chromene template. Due to their diverse biological activities, many of the thiophene derivatives are widely used as therapeutic agents as anticancer agents against various cancer cell lines.[22,23,24,25,26,27] it was planned to synthesize the thiophene/benzothiazole-4H-chromene hybrid with a view
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