Synthesis and D₂-like binding affinity of new derivatives of N3-[(1- ethyltetrahydro-1H-2-pyrrolyl)methyl]-4,5-dihydrobenzo[g]indole-3- carboxamide and related compounds

In previous papers 4a,b we have reported the syntheses and structure-activity relationships of a series of 5-phenyl-3-pyrrole carboxamide and related 4,5-dihydrobenzo[g]indole-3-carboxamide analogues whose most representative terms were 1a and 2a respectively. Encouraged by these results we carried out several modifications of 2a

Sintesi di 1,10-fenantroline chirali a simmetria C₂ derivati da monoterpeni naturali quali utili leganti per la catalisi asimmetrica

Nell’ambito dei leganti azotati, la sintesi di 1,10-fenantroline (phens) chirali ed il loro uso quali leganti chirali catalitici è stato poco investigato per le difficoltà incontrate nella preparazione dei più semplici analoghi a simmetria C2. Recentemente abbiamo riportato una nuova via sintetica per la preparazione di phens chirali a simmetria C2

Sintesi di nuovi leganti chirali dipiridilmetanici e loro applicazione nella sostituzione allilica palladio-catalizzata

In questo contesto, viene qui descritta la preparazione di nuove bispiridine chirali di tipo 2 e 3 formalmente ottenute per introduzione di una giunzione dimetilmetanica tra i due anelli piridinici di 1. Infine è stata investigata la capacità delle nuove bispiridine di influenzare la stereoselettività nella reazione di sostituzione allilica palladio-catalizzata. I risultati saranno riportati e discuss

Tricyclic pyrazoles: synthesis and biological evaluation of novel 4,5-dihydrobenzo-1h-6-oxa-cyclohepta[1,2-c] pyrazole-based analogues of the cannabinoid antagonist ness 0327

We report in this poster the synthesis and in vitro evaluation of novel 4,5- dihydrobenzo-1H-6-oxa-cyclohepta[1,2-c]pyrazoles 1Cb-l variously substituted in position 3

I 3,6-diazabiciclo[3.1.1]eptani: una nuova serie di potenti agonisti per i recettori µ degli oppioidi

In questa comunicazione presentiamo la sintesi di una nuova serie di diazabicicloalcani, i 3,6-diazabiciclo[3.1.1]eptani ed i preliminari dati biologici dei composti sintetizzati

RNAseq Analysis of Novel 1,3,4-Oxadiazole Chalcogen Analogues Reveals Anti-Tubulin Properties on Cancer Cell Lines

1,3,4-Oxadiazole derivatives are among the most studied anticancer drugs. Previous studies have analyzed the action of different 1,3,4-oxadiazole derivatives and their effects on cancer cells. This study investigated the characterization of two new compounds named 6 and 14 on HeLa and PC-3 cancer cell lines. Based on the previously obtained IC50, cell cycle effects were monitored by flow cytometry. RNA sequencing (RNAseq) was performed to identify differentially expressed genes, followed by functional annotation using gene ontology (GO), KEGG signaling pathway enrichment, and protein–protein interaction (PPI) network analyses. The tubulin polymerization assay was used to analyze the interaction of both compounds with tubulin. The results showed that 6 and 14 strongly inhibited the proliferation of cancer cells by arresting them in the G2/M phase of the cell cycle. Transcriptome analysis showed that exposure of HeLa and PC-3 cells to the compounds caused a marked reprograming of gene expression. Functional enrichment analysis indicated that differentially expressed genes were significantly enriched throughout the cell cycle and cancer-related biological processes. Furthermore, PPI network, hub gene, and CMap analyses revealed that compounds 14 and 6 shared target genes with established microtubule inhibitors, indicating points of similarity between the two molecules and microtubule inhibitors in terms of the mechanism of action. They were also able to influence the polymerization process of tubulin, suggesting the potential of these new compounds to be used as efficient chemotherapeutic agents

Oxadiazoles having antiproliferative activity

Oxadiazole derivatives of general formula (1) in which X, Y, R and R2 have the meanings defined in the disclosure. The compounds have antiproliferative activity against a number of human tumors cell lines and can therefore be used for the preparation of antitumor medicaments

Chiral pyridine <i>N</i>-oxides: useful ligands for asymmetric catalysis

The synthesis and applications in asymmetric catalysis of chiral pyridine N-oxide derivatives is reviewed

An Overview on different classes of viral entry and Respiratory Syncitial Virus (RSV) fusion inhibitors

The therapeutic approach to AIDS is based on the combination of different drugs in the highly active antiretroviral therapy (HAART) regimen. These drugs have a wide variety of side effects, and some strains of HIV can develop resistance: for these reasons new anti-HIV drugs are needed. In the wide field of anti-HIV medicine this review covers different classes of drugs which inhibit viral entry: in particular the classification of main categories, their mode of action and some new candidates for AIDS therapy are contemplated. Also covered in this review are respiratory syncytial virus (RSV) fusion inhibitors

Tricyclic Pyrazole-Based Compounds as Useful Scaffolds for Cannabinoid CB1/CB2 Receptor Interaction

Cannabinoids comprise different classes of compounds, which aroused interest in recent years because of their several pharmacological properties. Such properties include analgesic activity, bodyweight reduction, the antiemetic effect, the reduction of intraocular pressure and many others, which appear correlated to the affinity of cannabinoids towards CB1 and/or CB2 receptors. Within the search aiming to identify novel chemical scaffolds for cannabinoid receptor interaction, the CB1 antagonist/inverse agonist pyrazole-based derivative rimonabant has been modified, giving rise to several tricyclic pyrazole-based compounds, most of which endowed of high affinity and selectivity for CB1 or CB2 receptors. The aim of this review is to present the synthesis and summarize the SAR study of such tricyclic pyrazole-based compounds, evidencing, for some derivatives, their potential in the treatment of neuropathic pain, obesity or in the management of glaucoma