Mini-Reviews in Medicinal Chemistry, Vol 18, No 1 (2018)

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1,4-Benzothiazines- A biologically attractive scaffold

Mr. Amit Rai, Mr. Ashok K Singh, Mr. Vinit Raj, Dr. Sudipta Saha


1,4-benzothiazine (1,4-B), a pharmacophore of anti-psychotic drug phenothiazines, is a vital class of heterocyclic compounds implicating versatile biological activities. Among offering several interesting biological activities, 1,4-benzothiazines (1,4-Bs) have a tremendous ability to regulate diverse range of cellular pathways that can be explored for selective anticancer activity. Synthetic chemists have discovered numerous routes for the syntheses of various 1,4-B analogues that show excellent activities through multiple mechanisms. The direct comparison of activities with the parent 1,4-B derivative enables a systematic analysis of the structure activity relationship (SAR) among the series. Thus, the present review article offers a compilation and summarization of the synthetic strategies, biological activities and structure activity relationship concerning the bioactive heterocycle, 1,4-benzothiazine.


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