A couple of natural coumarins was identified in the seeds of two apples’ cultivars commonly known as Granny Smith and Red Delicious. The effect of the phenolic hydroxyl moieties found in these products was evaluated on the bioactivity. This evaluation included the structural alteration of these moieties into less hydrophilic ones to explore the significance of the parent moieties on the biological activity. The investigated biopotentials were antioxidant, antiproliferative, antibacterial, and antifungal effects. The antioxidant potential was investigated by detecting the ability of the natural and semisynthetic coumarins to trap the free hydroxyl and DPPH radicals. The antiproliferative potential was assessed via an MTT-depended assay versus eight cancerous-cell lines, included HeLa, SK-OV-3, AR42J, MCF-7, AB12, KYSE-30, LC540, and AMN3. The antibacterial potential was tested versus six common pathogenic bacterial strains via a well-defined disc diffusion assay. These pathogens were Escherichia coli, Salmonella typhi, Klebsiella pneumonia, Haemophilus influenzae, Shigella dysenteriae, and Pseudomonas aeruginosa. The antifungal potential was also screened by utilizing a similar microbiological technique versus three pathogenic fungi, involved Candida albicans, Aspergillus flavus, and Aspergillus niger. It is concluded that the investigated chemical moiety has a positive influence on the antioxidant and antiproliferative potentials of the natural derivatives, and a negative one on their antibacterial and antifungal potentials.

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

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