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Abstract

A series of substituted curcumin analogues have been designed and synthesized via condensation reaction of benzaldehydes and dehydroacetic acid. Synthesized molecules were further evaluated for their inhibitory activity against various cancer cell lines. Most of the synthesized compounds were significantly inhibited the growth of these cell lines. Ten most active compounds in the series were further screened to check their inhibitory effect 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 evaluated compounds reveals that among the synthesized compounds, nitro substituted chalcones 5 and 8 were the most active compounds having IC50 value of 5.49 and 4.46 μM against A549 (lung carcinoma) cell lines, respectively and significantly inhibited S. cervi Topoisomerase II activity upto more than 95 %.

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Curcumin Anticancer Topoisomerases II Chalcones

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Deepak Tripathi, V., & Kumar Shukla, A. (2018). Design and Synthesis of Novel Heterocyclic Curcumin Analogues as Anticancer Agents and Filarial Topoisomerase II Inhibitors. Asian Journal of Organic & Medicinal Chemistry, 3(4), 164–170. https://doi.org/10.14233/ajomc.2018.AJOMC-P149
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