The G-protein coupled receptors (GPCRs)
activated by free fatty
acids (FFAs) have emerged as new and exciting drug targets, due to
their plausible translation from pharmacology to medicines. This perspective
aims to report recent research about GPR120/FFAR4 and its involvement
in several diseases, including cancer, inflammatory conditions, and
central nervous system disorders. The focus is to highlight the importance
of GPR120 in Type 2 diabetes mellitus (T2DM). GPR120 agonists, useful
in T2DM drug discovery, have been widely explored from a structure–activity
relationship point of view. Since the identification of the first
reported synthetic agonist TUG-891, the research has paved the way
for the development of TUG-based molecules as well as new and different
chemical entities. These molecules might represent the starting point
for the future discovery of GPR120 agonists as antidiabetic drugs.
The search for human adenovirus (HAdV)-specific antiviral drugs for the treatment of HAdV infections in immunocompromised patients continues to be a challenging goal for medicinal chemistry. Here, we report the synthesis, biological evaluation, and structure-activity relationships of a small molecules library. We have identified six phenylpiperazine derivatives that significantly inhibited HAdV infection. These six compounds showed the capacity to block HAdV and, in addition, human cytomegalovirus (HCMV) replications at low micromolar concentration, with little or no cytotoxicity. On the basis of our biological studies, these molecules block HAdV and HCMV infections in different phases of their life cycle, providing potential candidates for the development of a new family of antiviral drugs for the treatment of infections by DNA viruses.
Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio-accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst. The in vitro assays, using a wide panel of human cancer cell lines showed, mainly for two novel regioisomer oleoyl-hybrids of quercetin, a remarkable increase in apoptotic cell populations. We suggested that the DNA damage shown as ɣH2AX signals might be the major cause of apoptotic cell death. Finally, we demonstrated convincing data about two novel polyphenol-based hybrids displaying a highly selective anti-cancer cytotoxicity and being superior compared to their reference/parental compounds.
A new backbone model for a chiral carbohydrate-derived ketone for asymmetric epoxidation is presented. The oxo function is sited in a seven-membered ring fused to the sugar moety. The synthesized compound is an effective chirality-
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