| Literature DB >> 26874345 |
Mohammed Al-Ghorbani1, Prabhu Thirusangu2, H D Gurupadaswamy1, V Girish1, H G Shamanth Neralagundi2, B T Prabhakar2, Shaukath Ara Khanum3.
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.Entities:
Keywords: Benzophenone-pyridine; CAD; DLA; Endonuclease
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Year: 2016 PMID: 26874345 DOI: 10.1016/j.bioorg.2016.02.001
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275