Design, Synthesis, and Evaluation of Novel Heterocyclic Compounds with Multi-Targeted Anticancer, Kinase Inhibitory, Antimicrobial and Anti-inflammatory Activities
DOI:
https://doi.org/10.29070/vrzexw52Keywords:
Design, Synthesis, Novel, Heterocyclic Compounds, Multi-Targeted Anticancer, Kinase Inhibitory, Antimicrobial, Anti-inflammatory ActivitiesAbstract
Heterocyclic compounds have long stood at the forefront of medicinal chemistry due to their remarkable pharmacological diversity and their presence in numerous therapeutic agents. This study outlines the design, synthesis, structural elucidation, and biological evaluation of a new series of heterocyclic derivatives, specifically focusing on three core scaffolds: 3,4-dihydro-2H-pyrrolo[3,4-b]quinazoline, 2-(4-bromo-2-chlorophenyl)-1,3-dihydro-2H-imidazo[4,5-b]pyridine, and 5-(phenylthio)-2-methyl-1,3,4-thiadiazole. These were rationally designed for activity against cancer, microbial infections, and inflammatory conditions. Characterization was carried out using ¹H/¹³C NMR, IR, and mass spectrometry, confirming the structural integrity of synthesized molecules. Cytotoxic testing showed that many quinazoline-based analogues inhibited kinases, including EGFR, HER2, and CDK2, and had strong inhibitory action against MCF-7 and A549 cell lines. Antimicrobial activity against both Gram-positive and Gram-negative bacteria was somewhat shown by imidazopyridine derivatives. The thiadiazole derivative showed anti-inflammatory potential by substantially inhibiting nitric oxide generation in RAW264.7 macrophages stimulated by LPS. According to structure-activity relationship (SAR) studies, the most important steps in increasing bioactivity were halogenation, sulfonamide inclusion, and electron-withdrawing substitutions. Future work includes scale-up synthesis, advanced SAR mapping, and mechanistic validation. This work underscores the utility of heterocyclic scaffolds in the development of multi-target therapeutic agents.
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