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

## TL;DR

This paper reports the synthesis of compounds with both anticancer and antiviral effects, showing promise against melanoma and viruses like SARS-CoV-2, Zika, and influenza.

## Contribution

The study introduces tricyclic compounds with dual anticancer and broad-spectrum antiviral activity against multiple epidemic-causing viruses.

## Key findings

- Compound 1 showed high anticancer activity with GI50 values between 1.54 μM and 2.03 μM in melanoma cell lines.
- Compound 13 exhibited strong anti-SARS-CoV-2 activity with a selectivity index of 150.00.
- Several compounds showed antiviral activity against influenza A and Zika viruses with notable selectivity indices.

## Abstract

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.