Arylpiperazinyl-Benzocycloheptapyrrole-Carboxamides Endowed with Dual Anticancer and Antiviral Activities.

In this work, we synthesized a small library of tricyclic compounds to assess whether they might have both anticancer and antiviral activity against three viruses that have recently caused epidemics. Concerning their anti-tumour activity, derivative 1 was found to be the compound with the highest GI50 values on some cancer cell line panels. Particularly, in melanoma cell lines, its GI50 values ranged between 1.54 μM (MALME-3M) and 2.03 μM (M14). Several derivatives with considerable anti-tumour activity showed antiviral activity as well, against influenza A virus (e.g., derivative 19, selectivity index of 21.36 in MDCK cells) or against Zika virus (compound 13, selectivity index of 20.20 in Huh-7 cells). Moreover, compounds 13 and 12 showed anti-SARS-CoV-2 activity, with selectivity indices of 150.00 and 63.63, respectively. Compound 1, for its anticancer activity, and 13, for its anti-SARS-CoV-2 activity, together with the compounds active against Zika virus and influenza A virus, are promising candidates for further studies.