AI Article Synopsis
- The text discusses new phenylpiperidine derivatives that act as inhibitors of QPCT and QPCTL.
- These compounds are presented as potential treatments for cancer and fibrotic diseases.
- The document also outlines methods for synthesizing these inhibitors.
Article Abstract
Provided herein are novel phenylpiperidine derivatives as QPCT and QPCTL inhibitors, pharmaceutical compositions, use of such compounds in treating cancer or fibrotic diseases, and processes for preparing such compounds.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11571085 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.4c00495 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Novel Phenylpiperidine Derivatives as QPCT and QPCTL Inhibitors for Treating Cancer or Fibrotic Diseases.
ACS Med Chem Lett
November 2024
Smith, Gambrell & Russell LLP, 1105 W. Peachtree Street NE, Suite 1000, Atlanta, Georgia 30309, United States.
Article Synopsis
- The text discusses new phenylpiperidine derivatives that act as inhibitors of QPCT and QPCTL.
- These compounds are presented as potential treatments for cancer and fibrotic diseases.
- The document also outlines methods for synthesizing these inhibitors.
Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy through the Activation of Antigen Presentation of cDC1 Cells.
J Med Chem
August 2024
School of Basic Medical Sciences, Fudan University, Shanghai 201210, China.
Aberrant activation of the Wnt/β-catenin signaling is associated with tumor development, and blocking β-catenin/BCL9 is a novel strategy for oncogenic Wnt/β-catenin signaling. Herein, we presented two novel β-catenin variations and exposed conformational dynamics in several β-catenin crystal structures at the BCL9 binding site. Furthermore, we identified a class of novel urea-containing compounds targeting β-catenin/BCL9 interaction.
View Article and Find Full Text PDFIdentification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.
ACS Med Chem Lett
February 2024
Research and Development, Bristol Myers Squibb, 700 Bay Road, Redwood City, California 94063, United States.
Small molecule toll-like receptor (TLR) 7 agonists have gathered considerable interest as promising therapeutic agents for applications in cancer immunotherapy. Herein, we describe the development and optimization of a series of novel TLR7 agonists through systematic structure-activity relationship studies focusing on modification of the phenylpiperidine side chain. Additional refinement of ADME properties culminated in the discovery of compound , which displayed nanomolar reporter assay activity and favorable drug-like properties.
View Article and Find Full Text PDFDiscovery of Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer.
J Med Chem
January 2023
Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, 285 Gebai Ni Road, Shanghai 201203, China.
Direct disruption of the β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction (PPI) is a potential strategy for colorectal cancer (CRC) treatment through inhibiting oncogenic Wnt activity. Herein, a series of 3-phenylpiperidine derivatives were synthesized and evaluated as β-catenin/BCL9 PPI inhibitors. Among them, compound showed the best IC (0.
View Article and Find Full Text PDFNovel dual-target μ‑opioid and TRPV1 ligands as potential pharmacotherapeutics for pain management.
Bioorg Chem
February 2023
School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China. Electronic address:
Currently, the development of effective analgesic drugs with few side effects remains a great challenge. Studies have suggested that multi-target drug treatments show high efficacy and reduced side effects compared to single-target drug therapies. In this work, we designed and synthesized two series of novel MOR/TRPV1 dual active ligands in which the phenylpiperidine group or the N-phenyl-N-(piperidin-4-yl) propionamide group as the MOR pharmacophore was fused to the benzylpiperazinyl urea-based TRPV1 pharmacophore.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!