Evidence map›Paper›PMID 37776573›Full record

ArticleEuropean journal of medicinal chemistry2023

Strategies for developing retinoic acid receptor alpha-selective antagonists as novel agents for male contraception.

Md Abdullah Al Noman, Rebecca A D Cuellar, Jillian L Kyzer, Sanny S W Chung, Narsihmulu Cheryala, Trinh A D Holth, Soma Maitra, Tahmina Naqvi, Henry L Wong, Ernst Schönbrunn and 3 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

7 citing papers in PubMed, 9 citations in OpenAlex.

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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

13 authors at 4 institutions in 1 country.

Md Abdullah Al NomanDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Rebecca A D CuellarDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Jillian L KyzerDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Sanny S W ChungDepartment of Genetics and Development, USA.
Narsihmulu CheryalaDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Trinh A D HolthDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Soma MaitraDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Tahmina NaqviDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Henry L WongDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Ernst SchönbrunnDepartment of Drug Discovery, Moffitt Cancer Center, 12902 USF Magnolia Drive, Tampa, FL, 33612, USA.
Jon E HawkinsonDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA.
Debra J WolgemuthDepartment of Genetics and Development, USA; Department of Obstetrics and Gynecology, USA; The Institute of Human Nutrition, USA; The Herbert Irving Comprehensive Cancer Center, Columbia University Medical Center, 1150 St. Nicholas Avenue, New York, NY, 10032, USA.
Gunda I GeorgDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, MN, 55414, USA. Electronic address: georg@umn.edu.
University of Minnesota · USColumbia University Irving Medical Center · USMoffitt Cancer Center · USPediatrics and Genetics · US

Funding

Drug Discovery & Synthesis of Contraceptive AgentsU01HD076542 · NICHD · UNIVERSITY OF MINNESOTA · PI GEORG, GUNDA I. · 2012 to 2016
$5.0M
Understanding Behavioral Patterns in Contraceptive UseU54HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI GEORG, GUNDA I. · 2017 to 2018
$4.4M
Chemistry-Biology Interface Training GrantT32GM008700 · NIGMS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI DISTEFANO, MARK D · 1999 to 2018
$4.0M
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 HD093540NICHD NIH HHS U01 HD076542NICHD NIH HHS U54 HD093540NIGMS NIH HHS T32 GM008700
6 · The paper itself

Abstract

Reported here are the synthesis and in vitro evaluation of a series of 26 retinoic acid analogs based on dihydronaphthalene and chromene scaffolds using a transactivation assay. Chromene amide analog 21 was the most potent and selective retinoic acid receptor α antagonist identified from this series. In vitro evaluation indicated that 21 has favorable physicochemical properties and a favorable pharmacokinetic PK profile in vivo with significant oral bioavailability, metabolic stability, and testes exposure. Compound 21 was evaluated for its effects on spermatogenesis and disruption of fertility in a mouse model. Oral administration of compound 21 at low doses showed reproducibly characteristic albeit modest effects on spermatogenesis, but no effects on fertility were observed in mating studies. The inhibition of spermatogenesis could not be enhanced by raising the dose and lengthening the duration of dosing. Thus, 21 may not be a good candidate to pursue further for effects on male fertility.

Indexed as

ContraceptionTestisAnimalsBenzopyransImidazolesMaleMiceRetinoic Acid Receptor alphaSulfonamidesThiophenesBenzopyranscompound 21ImidazolesRetinoic Acid Receptor alphaSulfonamidesThiophenesMale contraceptionRetinoic acid receptor alphaSelectivityStructure-activity relationships

Identifiers

PMID37776573
PMCPMC10841505
OpenAlexW4387008160

What OpenQuestion holds

Textmetadata
LicenceTDM
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.