Over the years, researchers
in drug discovery have taken advantage
of the use of privileged structures to design innovative hit/lead
molecules. The α-ketoamide motif is found in many natural products,
and it has been widely exploited by medicinal chemists to develop
compounds tailored to a vast range of biological targets, thus presenting
clinical potential for a plethora of pathological conditions. The
purpose of this perspective is to provide insights into the versatility
of this chemical moiety as a privileged structure in drug discovery.
After a brief analysis of its physical–chemical features and
synthetic procedures to obtain it, α-ketoamide-based classes
of compounds are reported according to the application of this motif
as either a nonreactive or reactive moiety. The goal is to highlight
those aspects that may be useful to understanding the perspectives
of employing the α-ketoamide moiety in the rational design of
compounds able to interact with a specific target.
We report here on the synthesis and multi-technique characterization of [Ru2Cl((2-phenylindol-3-yl)glyoxyl-L-leucine-L-phenylalanine)4] a novel diruthenium (II,III) complex obtained reacting [Ru2(μ-O2CCH3)4Cl] with a dual indolylglyoxylyl dipeptide anticancer agent. We soon realised that...
This article provides an overview of the various research approaches we have explored in recent years to improve metal-based agents for cancer or infection treatments. Although cisplatin, carboplatin, and oxaliplatin remain the cornerstones in tumor chemotherapy, the discovery and approval of novel inorganic anticancer drugs is a very slow process. Analogously, although a few promising inorganic drugs have found clinical application against parasitic or bacterial infections, their use remains relatively limited. Moreover, the discovery process is often affected by small therapeutic enhancements that are not attractive for the pharmaceutical industry. However, the availability of increasing mechanistic information for the modes of action of established inorganic drugs is fueling the exploration of various approaches for developing effective inorganic chemotherapy agents. Through a series of examples, some from our own research experience, we focus our attention on a number of promising strategies, including (1) drug repurposing, (2) the simple modification of the chemical structures of approved metal-based drugs, (3) testing novel drug combinations, and (4) newly synthesized complexes coupling different anticancer drugs. Accordingly, we aim to suggest and summarize a series of reliable approaches that are exploitable for the development of improved and innovative treatments.
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