With the aim of identifying the broad acting antiviral and anticancer agents, we discovered substituted aryl/heteroaryl derived thienyl chalcones as antiviral and anticancer agents. All thienyl chalcone derivaties II-VI displayed moderate to excellent antiviral activity towards several viruses tested. Compounds V and VI were turned out be active compounds towards human cytomegalovirus for both normal strain (AD169) as well as resistant isoloate (GDGr K17). Particularly, compound V showed very high potency (EC50: &lt;0.05 µM) towards AD169 strain of HCMV compared to standard drug Ganciclovir (EC50: 0.12 µM). Additionally, it showed moderate activity in secondary assay (AD169; EC50: 2.30 µM). The thienyl chalcone IV displayed high potency towards Rift Valley fever virus (RVFV) and Tacaribe virus (TCRV). Compound IV is nearly 28 times more potent in our initial in vitro visual assay (EC50: 0.39 μg/ml) and nearly 17 times more potent in neutral red assay (EC50: 0.71 μg/ml) compared to the standard drug Ribavirin (EC50: 11 μg/ml; visual assay and EC50: 12 μg/ml; neutral red assay). It is nearly 12 times more potent in our initial in vitro visual assay (EC50: &gt;1 μg/ml) and nearly 8 times more potent in neutral red assay (EC50: &gt;1.3 μg/ml) compared to the standard drug Ribavirin (EC50: 12 μg/ml; visual assay and EC50: 9.9 μg/ml; neutral red assay) towards Tacaribe virus (TCRV). Additionally, compound IV has shown strong growth inhibitory activity towards three major cancer (colon, breast and leukemia) cell lines and moderate growth inhibition shown towards other cancer cell lines screened. Compounds V and VI were demonstrated viral inhibition towards Human cytomegalovirus whereas compound IV towards Rift Valley fever virus and Tacaribe virus. Additionally, compound IV has displayed very good cytotoxicity towards colon, breast and leukemia cell lines in vitro.

Exploration of (hetero)aryl derived thienylchalcones for antiviral and anticancer activities

256th National Meeting (2018)

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