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Phenothiazine and its N-substituted derivatives are pivotal in heterocyclic chemistry, and serves as potential building blocks in chemical and pharmaceutical sciences. Over the past decade, extensive research has focused on the medicinal potentials of these compounds, exploring their anticancer, analgesic, anti-tumor, anti-inflammatory, and antibacterial properties. Due to their distinctive chemical compositions, phenothiazine and its N-substituted derivatives have facilitated the development of novel substitutions. This paper reviews recent advancements in the synthesis of phenothiazine and its N-substituted derivatives, with an emphasis on their potential biological roles. Numerous investigations have identified various types of phenothiazine and its N-substituted derivatives that exhibit compelling biological characteristics. It discusses the impact of different functional groups on phenothiazine at the N-substitution, specifically Cl, CF3, OH, N(C2H5)2, and (CH2)5CH3. Furthermore, the relationship between the biological activities and the structural characteristics of the compounds is examined, identifying the chemical groups and structural alterations that enhance bioactivity, reduce toxicity, and improve handling.
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