Design and Synthesis of Heterocyclic Curcumin Analogues as Filarial Topoisomerase II Inhibitors
Journal Title: Journal of Biological and chemical Chronicles - Year 2018, Vol 4, Issue 2
Abstract
A series of novel heterocyclic curcumin analogues (substituted cinnamoyl-4-hydroxy-6-methyl-2Hpyran- 2-one derivatives 3-24), were designed and synthesized via condensation of different benzaldehydes and dehydroacetic acid. A new way for modification of curcumin has been described in order achieves enhanced pharmacological properties. Synthesized derivatives were also evaluated for their inhibitory activity against filarial topoisomerase II enzyme. All the compounds screened against Topoisomerase II exhibited excellent inhibition upto percentage inhibition more than 95%. Further the structure–activity relationships of the cinnamoyl-4-hydroxy-6- methyl-2H-pyran-2-one derivatives (3-24) reveals that among the synthesized compounds, the nitro substituted chalcones derivatives 5 and 8 were the most active compounds by showing significant inhibition of S. cervi Topoisomerase II activity upto more than 95%.
Authors and Affiliations
Vishwa Deepak Tripathi, Anand Mohan Jha
Keywords
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