Pharmaceutical Sciences

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https://hdl.handle.net/20.500.11888/3211

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Browsing Pharmaceutical Sciences by Author "Haneen Marwan Abu Katab"

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    BIOLOGICAL EVALUATION OF 2-OXO-BENZOXAZOLE DERIVATIVES
    (2023-09-07) Haneen Marwan Abu Katab
    Benzoxazole derivatives are essential building blocks for innovative drugs due to their wide range of biological activities in medicinal chemistry, particularly their pharmacological effects (such as analgesic, antibacterial, antifungal, anti-inflammatory, and anticancer properties). The importance of benzoxazole derivatives in drug development is emphasized by this work, which also highlights their potential as therapeutic targets with a variety of pharmacological actions and structural flexibility. This study investigates the 1,3-oxazole nucleus, which is a very effective molecule with antibacterial, anticancer, analgesic, and anti-inflammatory characteristics. These substances are created both naturally and artificially by several organisms, including bacteria and marine life. Pharmaceutical compounds belonging to the 1,3-oxazole family can be used to synthesize a wide range of molecules with various therapeutic applications, such as antiviral and anticancer effects. The fascinating possibility of benzoxazole derivatives inhibiting anaerobic choline metabolism and their possible anticancer effects is examined in this work. Certain compounds based on benzoxazoles exhibit enhanced cytotoxicity, especially towards particular cancer cell lines, suggesting that they may be useful in stopping the spread of cancer cells. The promise of benzoxazole derivatives in pharmaceutical research is highly praised, and more investigation into the benzoxazole scaffold and its functionalization is encouraged to find more powerful and selective molecules with enhanced activity and decreased toxicity. The study's findings on sixteen artificial chemicals tested against seven cancer cell lines are presented in the article. The compounds BNZ-2, BNZ-4, BNZ-7, BNZ-9, and BNZ-10 show promise as anticancer agents. Key moieties, such as chlorobenzoyl, piperazine, piperidine, morpholinomethyl, and 4-methylpiperidin-1-yl, that are responsible for their actions against different cell lines are identified by a structural analysis using Structure-Activity Relationship (SAR) study. BNZ-10 has a lower IC50 value than other well-known anticancer medications, which suggests that it may be a more effective treatment against particular cancer cell types. It's important to remember, nevertheless, that doxorubicin (DOX) has far lower IC50 values than the majority of BNZ-1-16 drugs and is nonetheless a powerful anticancer agent. The study concludes by highlighting the tremendous promise of benzoxazole derivatives in drug development, particularly in the treatment of cancer, and the significance of particular structural motifs in controlling their biological activity. Novel treatment approaches in hepG2-associated malignancies require further research on molecular interactions and processes, especially those that affect hepG2 cells. The research advances the hunt for new medicines and helps to rationally develop anticancer drugs. Keywords: Benzoxazole Derivatives; Anticancer Efficacy; Structure-Activity Relationship (SAR); IC50 Values