Evidence map›Paper›PMID 33113810›Full record

ArticleInternational journal of molecular sciences2020

Discovery of Tricyclic Pyranochromenone as Novel Bruton's Tyrosine Kinase Inhibitors with in Vivo Antirheumatic Activity.

Hyewon Cho, Eun Lee, Hye Ah Kwon, Lee Seul, Hui-Jeon Jeon, Ji Hoon Yu, Jae-Ha Ryu, Raok Jeon

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.4field-weighted citation impact, top 37% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed, 7 citations in OpenAlex.

  1. Review
  2. Review
  3. The Development of BTK Inhibitors: A Five-Year Update.Molecules (Basel, Switzerland) · 2021
    Review
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 2 institutions in 1 country.

Hyewon ChoCollege of Pharmacy, Sookmyung Women's University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea.
Eun LeeCollege of Pharmacy, Sookmyung Women's University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea.
Hye Ah KwonCollege of Pharmacy, Sookmyung Women's University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea.
Lee SeulNew Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, 80 Chembok-ro, Dong-gu, Daegu 41061, Korea.
Hui-Jeon JeonNew Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, 80 Chembok-ro, Dong-gu, Daegu 41061, Korea.
Ji Hoon YuNew Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, 80 Chembok-ro, Dong-gu, Daegu 41061, Korea.
Jae-Ha RyuCollege of Pharmacy, Sookmyung Women's University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea.ORCID 0000-0002-6726-2297
Raok JeonCollege of Pharmacy, Sookmyung Women's University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea.ORCID 0000-0002-3857-4339
Sookmyung Women's University · KRDaegu-Gyeongbuk Medical Innovation Foundation · KR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Bruton's tyrosine kinase (BTK) is an attractive target for treating patients with B cell malignancies and autoimmune diseases. Many BTK inhibitors have been identified; however, like other kinase inhibitors, they lack diversity in their core structures. Therefore, it is important to secure a novel scaffold that occupies the adenine-binding site of BTK. We screened an in-house library of natural products and their analogs via a biochemical assay to identify a novel scaffold for targeting BTK. A pyranochromenone scaffold, derived from a natural active component decursin, was found to be effective at targeting BTK and was selected for further optimization. A series of pyranochromenone analogs was synthesized through the modification of pyranochromenone at the C7 position. Pyranochromenone compounds with an electrophilic warhead exhibited promising BTK inhibitory activity, with IC

Indexed as

Agammaglobulinaemia Tyrosine KinaseAnimalsAntirheumatic AgentsArthritis, ExperimentalBenzopyransBiological ProductsButyratesHumansMaleMice, Inbred DBAMolecular Docking SimulationMolecular StructureProtein DomainsProtein Kinase InhibitorsStructure-Activity RelationshipTHP-1 CellsAgammaglobulinaemia Tyrosine KinaseAntirheumatic AgentsBenzopyransBiological ProductsButyratesdecursinProtein Kinase InhibitorsBTK inhibitorirreversible inhibitorpyranochromenonerheumatoid arthritis

Identifiers

PMID33113810
PMCPMC7663272
OpenAlexW3094070676

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.