title: Synthesis and antiproliferative activity of benzophenone tagged pyridine analogues towards activation of caspase activated DNase mediated nuclear fragmentation in Dalton's lymphoma.
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.
authors.affiliation: Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Al-Ghorbani
authors.affiliation: Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (A), Kuvempu University, Shimoga 577203, Karnataka, India.
authors.forename: Prabhu
authors.initials: P
authors.lastname: Thirusangu
authors.affiliation: Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India.
authors.forename: H D
authors.initials: HD
authors.lastname: Gurupadaswamy
authors.affiliation: Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India.
authors.forename: V
authors.initials: V
authors.lastname: Girish
authors.affiliation: Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (A), Kuvempu University, Shimoga 577203, Karnataka, India.
authors.forename: H G
authors.initials: HG
authors.lastname: Shamanth Neralagundi
authors.affiliation: Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (A), Kuvempu University, Shimoga 577203, Karnataka, India.
authors.forename: B T
authors.initials: BT
authors.lastname: Prabhakar
authors.affiliation: Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India. Electronic address: shaukathara@yahoo.co.in.
authors.forename: Shaukath Ara
authors.initials: SA
authors.lastname: Khanum
mesh_terms: D000818:Animals; D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020169:Caspases / Q000378:metabolism*; D002467:Cell Nucleus / Q000187:drug effects* / Q000201:enzymology / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D003851:Deoxyribonucleases / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D005260:Female; D006801:Humans; D008223:Lymphoma / Q000235:genetics* / Q000473:pathology*; D051379:Mice; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D001577:Benzophenones; D011725:Pyridines; C047723:benzophenone; D003851:Deoxyribonucleases; D020169:Caspases; C023666:pyridine
keywords: Benzophenone-pyridine; CAD; DLA; Endonuclease