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

Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.

Journal of medicinal chemistry - 8 Jan 2015

Song Zilan, Yang Yanhong, Liu Zhiqing, Peng Xia, Guo Junfeng, Yang Xinying, Wu Kui, Ai Jing, Ding Jian, Geng Meiyu, Zhang Ao

Abstract excerpt

We have developed a series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) bearing a flexible amino acid side chain, different from the majority of the literature reported ALK inhibitors that often possess a structurally constrained arylpiperazine fragment or its equivalents in the solvent-interaction region. Extensive structural elaboration led to compound 15 possessing IC50 values of 2.7 and 15.3 nM,...

Read the complete abstract on PubMed

Topics

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

Share to Anaplastic Lymphoma Kinase
Share to Area Under Curve

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Discovery

Share to Models, Chemical

Share to NIH 3T3 Cells

Share to Sulfones

Share to Tumor Burden

Share to Xenograft Model Antitumor Assays

Source

Identifiers

PMID: 24785465
DOI: 10.1021/jm5005144

Genes

ALK

Variants

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

Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.PMID 24785465Read ↗

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 ↗

Design, synthesis and antitumor evaluation of ATP dual-mimic 2,4-diarylaminopyrimidine and aminoindazole conjugates as potent anaplastic lymphoma kinase inhibitors.Semantic proximity Read ↗

Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.Semantic proximity Read ↗

Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations.Semantic proximity Read ↗

Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.Semantic proximity Read ↗

Identification of highly potent 2,4-diarylaminopyrimidine analogs of a typical piperidinyl-4-ol moiety as promising antitumor ALK inhibitors.Semantic proximity Read ↗

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

Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.Semantic proximity Read ↗

Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.Semantic proximity Read ↗

Identification of non-ATP-competitive α-carboline inhibitors of the anaplastic lymphoma kinase.Semantic proximity Read ↗

Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects.Semantic proximity Read ↗

Identification of type II inhibitors targeting BRAF using privileged pharmacophores.Semantic proximity Read ↗

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