Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Identification of 6,9-dihydro-5H-pyrrolo[3,2-h]quinazolines as a new class of F508del-CFTR correctors for the treatment of cystic fibrosis.

European journal of medicinal chemistry - 5 Oct 2024

Barreca Marilia, Renda Mario, Spanò Virginia, Montalbano Alessandra, Raimondi Maria Valeria, Giuffrida Stefano, Bivacqua Roberta, Bandiera Tiziano, Galietta Luis J V, Barraja Paola

Abstract excerpt

Although substantial advances have been obtained in the pharmacological treatment of cystic fibrosis (CF) with the approval of Kaftrio, a combination of two correctors (VX-661, VX-445) and one potentiator (VX-770), new modulators are still needed to rescue F508del and other CFTR mutants with trafficking defects. We have previously identified PP compounds based on a tricyclic core as correctors with high efficacy...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Cystic Fibrosis
Share to Cystic Fibrosis Transmembrane Conductance Regulator

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Dose-Response Relationship, Drug

Share to Molecular Structure

Share to Mutation

Share to Pyrroles

Share to Quinazolines

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 39089001
DOI: 10.1016/j.ejmech.2024.116691

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Identification of 6,9-dihydro-5H-pyrrolo[3,2-h]quinazolines as a new class of F508del-CFTR correctors for the treatment of cystic fibrosis.PMID 39089001Read ↗

Novel tricyclic pyrrolo-quinolines as pharmacological correctors of the mutant CFTR chloride channel.Semantic proximity Read ↗

Synthesis and Biological Evaluation of Pyrazole-Pyrimidones as a New Class of Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR).Semantic proximity Read ↗

Structure-guided combination of novel CFTR correctors to improve the function of F508del-CFTR in airway epithelial cells.Semantic proximity Read ↗

Novel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.Semantic proximity Read ↗

Evaluation of Fused Pyrrolothiazole Systems as Correctors of Mutant CFTR Protein.Semantic proximity Read ↗

Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis.Semantic proximity Read ↗

Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.Semantic proximity Read ↗

Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.Semantic proximity Read ↗

Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.Semantic proximity Read ↗

Identification of novel F508del-CFTR traffic correctors among triazole derivatives.Semantic proximity Read ↗

Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy.Semantic proximity Read ↗

Molecular Docking and QSAR Studies as Computational Tools Exploring the Rescue Ability of F508del CFTR Correctors.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.