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

Late-stage modification of complex drug: Base-controlled Pd-catalyzed regioselective synthesis and bioactivity of arylated osimertinibs.

Science advances - 8 Mar 2024

Feng Rui, Zhen Yong-Qi, Wu Dongbo, Sun Lian, Xu Jin-Bu, Li Xiaohuan, Zhang Lan, Gao Feng

Abstract excerpt

Achieving regioselective synthesis in complex molecules with multiple reactive sites remains a tremendous challenge in synthetic chemistry. Regiodivergent palladium-catalyzed C─H arylation of complex antitumor drug osimertinib with various aryl bromides via the late-stage functionalization strategy was demonstrated here. This reaction displayed a switch in regioselectivity under complete base control. Potassium...

Read the complete abstract on PubMed

Topics

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

Share to Acrylamides
Share to Aniline Compounds

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Catalysis

Share to ErbB Receptors

Share to Indoles

Share to Lung Neoplasms

Share to Protein Kinase Inhibitors

Share to Pyrimidines

Source

Open in PubMed Open full text

Identifiers

PMID: 38457511
DOI: 10.1126/sciadv.adl0026
PMCID: PMC10923520

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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

Late-stage modification of complex drug: Base-controlled Pd-catalyzed regioselective synthesis and bioactivity of arylated osimertinibs.PMID 38457511Read ↗

Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.Semantic proximity Read ↗

Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.Semantic proximity Read ↗

The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations.Semantic proximity Read ↗

Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.Semantic proximity Read ↗

Design, synthesis and biological evaluation of imine-containing inhibitors against the triple-mutant EGFR kinases based on the scaffold of osimertinib.Semantic proximity Read ↗

Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors.Semantic proximity Read ↗

Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation.Semantic proximity Read ↗

Design, synthesis and biological evaluation of 2-phenylaminopyrimidine derivatives as EGFR inhibitors.Semantic proximity Read ↗

Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants.Semantic proximity Read ↗

Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors.Semantic proximity Read ↗

Catalytic Lysine745 targeting strategy in fourth-generation EGFR tyrosine kinase inhibitors to address C797S mutation resistance.Semantic proximity Read ↗

Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.Semantic proximity Read ↗

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