Abstract
Series of 4H-chromone-based hydrazones 3a-z, pyrazolecarboxylates 5a-x and pyrazolylmethanones 6a-u were prepared and screened for their anti-proliferative activity on A549, HeLa, DU145 and MDAMB 231 cell lines. The hydrazone compound 3s with a chloro substituent on the chromanone moiety and a methoxy group on the phenyl ring displayed promising activity on A549, HeLa and DU145 cell lines. The compound 5p with a bromo substituent on the chromanone moiety and a methyl group on the phenyl ring displayed potent activity on DU145. Furopyrazolecarboxylate 5w having a methyl substituent on the phenyl ring displayed potent activity on HeLa cell line. The pyrazolylmethanone 6e with a fluoro substituent on the phenyl ring and compound 6j having a methyl substituent on the chromanone moiety and a methoxy group on the phenyl ring have shown promising anti-proliferative activity on HeLa cell line.
Highlights
Hydrazones, pyrazoles and pyrazolylmethanones are important heterocyclic compounds.[1]
In the course of our efforts in discovery and identification of biologically active compounds,[9,10,11,12] we focused research on 3-formylchromones and prepared series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates.[13]
The present manuscript describes the preparation of 3-formylchromone-based hydrazones, pyrazolecarboxylates, pyrazolylmethanones and their anti-proliferative activity
Summary
Hydrazones, pyrazoles and pyrazolylmethanones are important heterocyclic compounds.[1]. Celebrex is a COX-2 selective non-steroidal anti-inflammatory drug used to treat the pain and inflammation.[6] Sildenafil is a pharmaceutical drug used to treat erectile dysfunction.[7] Pyrazolylmethanones prepared by the reduction of carboxaldehydes were found to be anti-microbial and anti-inflammatory agents.[8]. In the course of our efforts in discovery and identification of biologically active compounds,[9,10,11,12] we focused research on 3-formylchromones and prepared series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates.[13] Further, pyridine, pyridone and benzopyridocarboxylates were reported by three-component, one-pot reaction of 3-formylchromones, benzylamines, 2-aminophenols with 3-oxobutanoates.[14] The present manuscript describes the preparation of 3-formylchromone-based hydrazones, pyrazolecarboxylates, pyrazolylmethanones and their anti-proliferative activity
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