Synthesis, structural characterization and biological evaluation of novel [1,2,4]triazolo [1,5-b][1,2,4]benzothiadiazine-benzothiazole conjugates as potential anticancer agents |
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| Authors: | Kamal Ahmed Khan M Naseer A Reddy K Srinivasa Srikanth Y V V Sridhar B |
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| Institution: | 1. Chemical Biology, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 2. 007, India;3. Corresponding author: Ahmed Kamal, e‐mail: ahmedkamal@iict.res.in;4. Laboratory of X‐ray Crystallography, Indian Institute of Chemical Technology, Hyderabad 500 007, India |
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| Abstract: | Two series of 10-substituted 5,5-dioxo-5,10-dihydro1,2,4]triazolo1,5-b]1,2,4]benzothiadiazine 2-methyl/ethyl sulfanyl benzothiazole derivatives (5a-d) and 10-substituted 5,5-dioxo-5,10-dihydro1,2,4]triazolo1,5-b]1,2,4] benzothiadiazine 2-phenoxy benzothiazole derivatives (16a-c) were synthesized and their structures confirmed by NMR, MS, IR and X-ray crystallography. These compounds were evaluated for their cytotoxicity against 60 human tumour cell lines. One of the synthesized compounds (5b) exhibited significant inhibitory activity against most of the cell lines and has been further evaluated for the five-dose screening. |
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| Keywords: | [1 2 4]triazolo[1 5‐b][1 2 4]benzothiadiazines anticancer activity benzothiazoles X‐ray crystallography |
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