Protein Kinases (PKs) are a heterogeneous family of enzymes that modulate several biological
pathways, including cell division, cytoskeletal rearrangement, differentiation and apoptosis. In particular,
due to their crucial role during human tumorigenesis and cancer progression, PKs are ideal targets
for the design and development of effective and low toxic chemotherapeutics and represent the second
group of drug targets after G-protein-coupled receptors. Nowadays, several compounds have
been claimed to be PKs inhibitors, and some of them, such as imatinib, erlotinib and gefitinib, have already
been approved for clinical use, whereas more than 30 others are in various phases of clinical trials.
Among them, some natural or synthetic carbazole-based molecules represent promising PKs inhibitors
due to their capability to interfere with PK activity by different mechanisms of action including
the ability to act as DNA intercalating agents, interfere with the activity of enzymes involved in DNA
duplication, such as topoisomerases and telomerases, and inhibit other proteins such as cyclindependent
kinases or antagonize estrogen receptors. Thus, carbazoles can be considered a promising
this class of compounds to be adopted in targeted therapy of different types of cancer.