Evidence map›Paper›PMID 40120495›Full record

ArticleEuropean journal of medicinal chemistry2025

Macrocyclic dihydropyridine analogs as pan-BET BD2-preferred inhibitors.

Jiewei Jiang, Taimeng Liang, Jonathan Solberg, Alice Chan, Prakriti Kalra, Rui Shi, William C K Pomerantz, Jon E Hawkinson, Ernst Schönbrunn, Gunda I Georg

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. Unusual backfolded binding poses of BAZ2A bromodomain binders.Acta crystallographica. Section D, Structural biology · 2026
    Article
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

10 authors.

Jiewei JiangDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, MN, 55414, USA.
Taimeng LiangDepartment of Chemistry, University of Minnesota, 207 Pleasant St. SE, Minneapolis, MN, 55455, USA.
Jonathan SolbergDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, MN, 55414, USA.
Alice ChanMoffitt Cancer Center, Department of Drug Discovery, 12902 Magnolia Drive, Tampa, Fl, 33612, USA.
Prakriti KalraDepartment of Chemistry, University of Minnesota, 207 Pleasant St. SE, Minneapolis, MN, 55455, USA.
Rui ShiDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, MN, 55414, USA.
William C K PomerantzDepartment of Chemistry, University of Minnesota, 207 Pleasant St. SE, Minneapolis, MN, 55455, USA.
Jon E HawkinsonDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, MN, 55414, USA.
Ernst SchönbrunnMoffitt Cancer Center, Department of Drug Discovery, 12902 Magnolia Drive, Tampa, Fl, 33612, USA.
Gunda I GeorgDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, MN, 55414, USA. Electronic address: georg@umn.edu.

Funding

Understanding Behavioral Patterns in Contraceptive UseP50HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI GEORG, GUNDA I. · 2019 to 2020
$3.9M
NICHD NIH HHS HHSN275201300017CNICHD NIH HHS HHSN275201300017INICHD NIH HHS P50 HD093540
6 · The paper itself

Abstract

Starting from dihydropyridopyrimidine benzyl ester 1, we pursued a macrocyclization strategy by linking its two aryl rings, hypothesizing that decreasing the conformational flexibility of the ester side chain would increase bromodomain and extra-terminal (BET) protein affinity and selectivity. We prepared 14 analogs and tested them in our fluorescent polarization (FP) assay for BRDT-1 and BRD4-1 affinity. Based on their K

Indexed as

Antineoplastic AgentsDihydropyridinesMacrocyclic CompoundsNuclear ProteinsTranscription FactorsBromodomain Containing ProteinsCell Cycle ProteinsCell Line, TumorCell ProliferationDose-Response Relationship, DrugHumansMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsBRD4 protein, humanBromodomain Containing ProteinsCell Cycle ProteinsDihydropyridinesMacrocyclic CompoundsNuclear ProteinsTranscription FactorsBromodomain 2InhibitorsMacrocyclesMultiple myeloma MM.1S

Identifiers

PMID40120495
PMCPMC11993331

What OpenQuestion holds

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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.