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Carbazole Derivatives as Kinase-Targeting Inhibitors for Cancer Treatment

[ Vol. 20 , Issue. 6 ]

Author(s):

Jessica Ceramella, Domenico Iacopetta, Alexia Barbarossa, Anna Caruso*, Fedora Grande*, Maria Grazia Bonomo, Annaluisa Mariconda, Pasquale Longo, Saturnino Carmela and Maria Stefania Sinicropi   Pages 444 - 465 ( 22 )

Abstract:


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.

Keywords:

Protein kinases, kinases inhibitors, carbazoles, anticancer drugs, targeted therapy, cancer.

Affiliation:

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS), Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS), Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS), Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS), Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS), Department of Science, University of Basilicata, 85100 Potenza, Department of Science, University of Basilicata, 85100 Potenza, Department of Biology and Chemistry, University of Salerno, 84084 Fisciano, Department of Science, University of Basilicata, 85100 Potenza, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, (CS)

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