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 ac-
tivity 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.