Design and Synthesis of Heterocyclic Curcumin Analogues as Filarial Topoisomerase II Inhibitors

Author(s): Vishwa Deepak Tripathi* & Anand Mohan Jha

A series of novel heterocyclic curcumin analogues (substituted cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-onederivatives 3-24), were designed and synthesized via condensation of different benzaldehydes and de-hydroacetic acid. A new way for modification of curcumin has been described in order achieves enhanced pharma-cological properties. Synthesized derivatives were also evaluated for their inhibitory activity against filarial topoi-somerase II enzyme. All the compounds screened against Topoisomerase II exhibited excellent inhibition upto per-centage inhibition more than 95%. Further the structureactivity relationships of the cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-onederivatives (3-24) reveals that among the synthesized compounds, the nitro substituted chal-cones derivatives 5 and 8 were the most active compounds by showing significant inhibition of S. cerviTopoisom-erase II activity upto more than 95%.


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