The first phosphoric acid-catalyzed asymmetric direct arylative reactions of 2-naphthols with quinone derivatives have been developed, providing efficient access to a class of axially chiral biaryldiols in good yields with excellent enantioselectivities under mild reaction conditions. This approach is a highly convergent and functional group tolerant route to the rapid construction of axially chiral compounds from simple, readily available starting materials. The excellent stereocontrol of the process stems from efficient transfer of stereochemical information from the chiral phosphoric acid into the axis chirality of the biaryldiol products. Preliminary results demonstrate that the biaryldiols can act as efficient chiral ligands in asymmetric transformations.
The first phosphoric acid catalyzed direct arylation of 2-naphthylamines with iminoquinones for the atroposelective synthesis of axially chiral biaryl amino alcohols has been developed. This reaction constitutes a highly functional-group-tolerant route for the rapid construction of enantioenriched axially chiral biaryl amino alcohols, and is a rare example of 2-naphthylamines acting as nucleophiles in an organocatalytic enantioselective transformation. Furthermore, the products, which feature various halogen atoms, provide access to structurally diverse axially chiral amino alcohols through further transformations.
Purpose: To investigate the risk factors for progression to castration-resistant prostate cancer (CRPC) in metastatic prostate cancer (mPCa) patients who underwent androgen deprivation therapy (ADT).Methods: We analyzed 216 patients with mPCa who underwent ADT between January 2006 and December 2015 at the First Affiliated Hospital of Fujian Medical University. Univariate and multivariate Cox regression analysis were used to explore the risk factors for progression to CRPC. Kaplan-Meier analysis and log-rank test were used to evaluate the difference in progression-free survival (PFS).Results: A total of 121 (56.0%) patients who underwent ADT showed progression to CRPC. Multivariate Cox regression analysis demonstrated that Gleason grade group, prostate-specific antigen nadir (nPSA), and time to PSA nadir (TTN) were risk factors for progression to CRPC in mPCa patients. Kaplan-Meier analysis demonstrated that patients in Gleason grade group ≥3, nPSA >0.2 ng/ml and TTN <6 months had shorter PFS.Conclusion: This study demonstrated that Gleason grade group, nPSA and TTN were risk factors for progression to CRPC. Patients with higher Gleason grade group, higher nPSA and shorter TTN have shorter PFS and higher risk of progression to CRPC after ADT.
Testicular cancer is the most common solid malignancy among young men. We downloaded data of testicular cancer patients from The Cancer Genome Atlas database to find novel genes in the testicular cancer microenviroment based on ESTIMATE algorithm-derived immune scores. A total of 156 cases of testicular cancer were included in this study and 165 cases of normal testicular tissues were used. We divided the testicular cancer patients into high-and low-score groups based on their immune scores. We identified 1,226 differentially expressed genes (fold change > 2, false discovery rate < 0.05), including 688 downregulated genes and 538 upregulated genes, between these two groups. The top Gene Ontology terms were involved in the immune response-regulating cell surface receptor signaling pathway, immune response-activating cell surface receptor signaling pathway, external side of the plasma membrane, and receptor ligand activity. By performing the Kyoto Encyclopedia of Genes and Genomes analysis, we demonstrated that cAMP signaling pathway was highly enriched among these differentially expressed genes. High expression of LINC01564, LINC02208, ODAM, RNA5SP111, and RNU6-196P were found to be associated with poor overall survival. The expression of genes was further validated by the Human Protein Atlas and only ALB and IFNG were demonstrated to be differentially expressed between testis tissue and testicular cancer tissue.
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