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

• Novel benzophenone tagged pyridine derivatives 8a–l were synthesized in good yield.
• All the synthesized compounds were characterized by spectral studies and elemental analysis.
• Also, in vitro and in vivo antiproliferative of compounds 8a–l against DLA cells were studies.
• Among the series, compounds 8b and 8e displayed potent antiproliferative effect.

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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