Diarylureas as Antitumor Agents

Abstract

The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come into the market as an anticancer agent was sorafenib, followed by some others. In this review, we survey progress over the past 10 years in the development of new diarylureas as anticancer agents.

Searching for Small Molecules as Antibacterials: Non-Cytotoxic Diarylureas Analogues of Triclocarban

“…Triclocarban, N-(4-chlorophenyl)-N'- (3,4-dichlorophenyl)urea, is a highly effective and broad spectrum antimicrobial that has been successfully used in personal care products for over 60 years [3]. It belongs to the privileged class of diarylureas, which have been recently extensively reviewed for their multiple actions, including the anticancer [4], and have also been proposed for a repositioning as antimicrobial agents and/or for the treatment of new pandemics, including COVID-19 [5,6]. It is predominantly found in household necessities and personal care products, especially dermal cleaning products such as antibacterial bar/liquid soap, body lotion, deodorants, aftershave soaps, hand sanitizers, toothpaste, handwash and mouthwash [7].…”

Special Issue on “Anticancer Drugs Activity and Underlying Mechanisms”

“…Again, Catalano et al [24] reviewed the different properties of diarylureas [8,25], namely ureas bearing two aromatic moieties as substituents, focusing on their role as important pharmacophore in anticancer drugs over the past 10 years. A clinically used member of this class, sorafenib was the lead compound approved from Food and Drug Administration (FDA) and the European Medicinal Agency (EMEA) for the treatment of advanced metastatic hepatocellular carcinoma and advanced renal cell carcinoma, paving the way to other diarylureas derivatives, such as regorafenib, linifanib, tivozanib and ripretinib, which share the ability to inhibit the kinases.…”

A Review on the Advancements in the Field of Metal Complexes with Schiff Bases as Antiproliferative Agents

“…Complexes containing the transition metals platinum, gold and silver have attracted much attention due to their antitumor effects. Schiff bases, as well as diarylureas [8][9][10], have been defined as "privileged" ligands in organic synthesis, thanks to their affordability, easy synthesis and different biological activities and ability to form complexes with almost all metals [11][12][13]. Actually, they may form complexes with transition metals, platinum group metals (PGM) [14], lanthanides [15,16], and actinides [17,18] and many of them have been extensively described in the literature [19,20].…”