In:
ChemistrySelect, Wiley, Vol. 6, No. 42 ( 2021-11-15), p. 11822-11831
Abstract:
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 ( 1 H and 13 C), 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)‐1 H ‐pyrazol‐4‐yl)‐3‐(2,4,6‐trimethoxyphenyl)prop‐2‐en‐1‐one ( 4 j ) displayed good cytotoxicity with IC 50 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)‐1 H ‐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.
Type of Medium:
Online Resource
ISSN:
2365-6549
,
2365-6549
DOI:
10.1002/slct.202103375
Language:
English
Publisher:
Wiley
Publication Date:
2021
detail.hit.zdb_id:
2844262-3
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