Synthesis and antiproliferative activity of benzophenone tagged pyridine analogues towards activation of caspase activated DNase mediated nuclear fragmentation in Dalton’s lymphoma

Al-Ghorbani, Mohammed and Thirusangu, Prabhu and Gurupadaswamy, H. D. and Girish, V. and Shamanth Neralagundi, H. G. and Prabhakar, B. T. and Khanum, Shaukath Ara (2016) Synthesis and antiproliferative activity of benzophenone tagged pyridine analogues towards activation of caspase activated DNase mediated nuclear fragmentation in Dalton’s lymphoma. Bioorganic Chemistry, 65. 73 - 81.

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Official URL: https://doi.org/10.1016/j.bioorg.2016.02.001

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.

Item Type: Article
Uncontrolled Keywords: Benzophenone-pyridine, DLA, CAD, Endonuclease
Subjects: C Chemical Science > Chemistry
Divisions: Yuvaraj college > Chemistry
Depositing User: manjula User
Date Deposited: 21 Jun 2019 11:16
Last Modified: 21 Jun 2019 11:16
URI: http://eprints.uni-mysore.ac.in/id/eprint/3630

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