Synthesis and antiproliferative activity of benzophenone tagged pyridine analogues towards activation of caspase activated DNase mediated nuclear fragmentation in Dalton’s lymphoma |
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| Institution: | 1. Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (Autonomous), Kuvempu University, Shivamogga 577203, Karnataka, India;2. Laboratory for Immunomodulation and Inflammation Biology, Department of Studies and Research in Biochemistry, Sahyadri Science College (Autonomous), Kuvempu University, Shivamogga 577203, Karnataka, India;3. Postgraduate Department of Studies and Research in Biotechnology & Bioinformatics, Kuvempu University, Shankaraghatta, Shivamogga 577203, Karnataka, India |
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| Abstract: | A series of benzophenones possessing pyridine nucleus 8a–l were synthesized by multistep reaction sequence and evaluated for antiproliferative activity against DLA cells by in vitro and in vivo studies. The results suggested that, compounds 8b with fluoro group and 8e with chloro substituent at the benzoyl ring of benzophenone scaffold as well as pyridine ring with hydroxy group exhibited significant activity. Further investigation in mouse model suggests that compounds 8b and 8e have the potency to activate caspase activated DNase (endonuclease) which is responsible for DNA fragmentation, a primary hallmark of apoptosis and thereby inhibits the Dalton’s lymphoma ascites tumour growth. |
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| Keywords: | Benzophenone-pyridine DLA CAD Endonuclease |
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