A series of new quinoline pyrazolyl‐chalcone hybrids (4 a–4 s) was obtained from 4‐acetyl‐5‐methylquinolylpyrazole and aromatic aldehydes and the structure of these hybrids were established with the help of FTIR, 1D NMR (1H and 13C), 2D NMR and HRMS data. The anticancer potential of selected quinoline pyrazolyl‐chalcone hybrids was evaluated against colon cancer (HT‐29, HCT‐116), lung cancer (A549), and prostate cancer (PC‐3) cell lines. (E)‐1‐(5‐Methyl‐1‐(4‐methylquinolin‐2‐yl)‐1H‐pyrazol‐4‐yl)‐3‐(2,4,6‐trimethoxyphenyl)prop‐2‐en‐1‐one (4 j) displayed good cytotoxicity with IC50 values of 5.4, 3.2 and 2.8 μM against HT‐29, A549, and PC‐3 cancer cell lines, respectively. The antimicrobial potential of quinoline pyrazolyl‐chalcone hybrids was tested against three bacterial strains (B. subtilis, S. aureus and E. coli) and two fungal strains (A. niger and C. albicans). (E)‐1‐(5‐Methyl‐1‐(4‐methylquinolin‐2‐yl)‐1H‐pyrazol‐4‐yl)‐3‐(3‐nitrophenyl)prop‐2‐en‐1‐one (4 r) exhibited significant activity against Gram positive bacteria (B. subtilis and S. aureus) and fungal strains with MIC value of 15.6 μM. Molecular docking analysis was conducted to determine the binding interactions of quinoline pyrazolyl‐chalcone hybrids with their respective biochemical targets viz. Epidermal growth factor receptor tyrosine kinase (EGFR), Thymidylate kinase (TMK) and C. albicans N‐myristoyltransferase.
A series of furo[3,2-c]pyrones and furo[3,2-c]coumarins agents were efficiently synthesized and structure recognizable proof was performed by FTIR and NMR. The furo[3,2-c]pyrones and furo[3,2-c]coumarins were evaluated against three bacterial strains (Bacillus subtilis, Staphylococcus aureus and Escherichia coli) and two parasitic strains (Aspergillus niger and Candida albicans). The antimicrobial results demonstrated that a couple of compounds showed noteworthy outcomes relating to the standard medications. Compounds 6 b and 9 f indicated great action against Escherichia coli and Bacillus subtilis with MIC value 0.0108 μmol/ml and 0.0120 μmol/ml, respectively. Compound 9 f also showed better activity against fungal strains with MIC value 0.0120 μmol/ml. Based on the outcomes of antimicrobial activities, docking study was performed to know the binding interface of furo[3,2-c]pyrones and furo[3,2-c] coumarins with DNA gyrase topoisomerase II.
Synthesis of a number of highly oxygenated furo [3,2-c]pyran/chromen-4-one has been accomplished by one-pot reaction from easily available dehydroacetic acid/3-acetyl-4-hydroxycoumarin or their chalcones and α-bromoketones. All the synthesized molecules were characterized utilizing various spectroscopic techniques and screened for anticancer activity (in vitro) against three colon (HCT-116, SW-620, HT-24), lung (A-549), prostate-(PC-3), breast (MCF-7) cell lines. Compounds 5a, 9d, 9f showed good activity against breast MCF-7 cancer cell line having IC 50 values 6.9, 2.8, 5.3 μM, respectively. Of these compounds, 9d showed better activity against prostate PC-3 cell line with IC 50 value 3.8 μM. The synthesized compounds were also studied for antibacterial activity (in vitro) using different strains of bacteria (Bacillus subtilis and Staphylococcus aureus -Gram-positive and Escherichia coli, Pseudomonas aeruginosa -Gram negative) as well as fungal strains (Aspergillus niger and Candida albicans) using Norfloxacin and Fluconazole as antibacterial and antifungal standard drugs, respectively. The antimicrobial screening study showed that compound 9f exhibited promising activity against S. aureus and B. subtilis, while 5h showed excellent and 5i and 9b showed better activity against E. coli. Compounds 5d and 5e showed promising activity against P. aeruginosa. The compounds 5c-5e displayed excellent activity against C. albicans and A. niger than Fluconazole.
Synthesis of a number of highly oxygenated furo[3,2-c]pyran-4-one (4, 5) and furo[3,2-c]chromen-4-one (8, 9) has been accomplished by a simple one pot reaction from easily available versatile starting materials - dehydroacetic acid and 3-acetyl-4-hydroxycoumarin. All the synthesized molecules were characterized utilizing various spectroscopic techniques and screened for anticancer activity (in vitro) against three Colon (HCT-116, SW-620, HT-24), Lung (A-549), Prostate-(PC-3), Breast-(MCF-7) cell lines. Compounds 5a, 9d, 9f showed good activity against breast MCF-7 cancer cell line having IC50 values 6.9, 2.8, 5.3 µM, respectively. Out of these compound 9d showed better activity against prostate PC-3 cell line with IC50 value 3.8 µM. The synthesized compounds were also studied for potential antibacterial activity (in vitro) using different strains of bacteria (Bacillus subtilis and Staphylococcus aureus -Gram-positive, and Escherichia coli- Gram negative) as well as fungal strains (Aspergillus niger and Candida albicans) using Norfloxacin and Fluconazole as antibacterial and antifungal standard drugs, respectively. The outcome of the antimicrobial screening study showed that compound 9f exhibited promising activity against S. aureus and B. subtilis while 5h showed excellent and 5i and 9b showed better activity against E. coli. The compounds 5c-5e displayed excellent activity against C. albicans and A. niger than Fluconazole.
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