Evidence map›Paper›PMID 27933964›Full record

ArticleJournal of medicinal chemistry2016

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).

Chunkai Wang, Qingjie Zhao, Mireille Vargas, Jeremy O Jones, Karen L White, David M Shackleford, Gong Chen, Jessica Saunders, Alice C F Ng, Francis C K Chiu and 4 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
3.3field-weighted citation impact, top 7% 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

9 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Cu-catalyzedOrganic letters · 2020
    Article
  6. Review
  7. SAR of a new antischistosomal urea carboxylic acid.Bioorganic & medicinal chemistry letters · 2018
    Article
  8. Progress in antischistosomal N,N'-diaryl urea SAR.Bioorganic & medicinal chemistry letters · 2018
    Article
  9. 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

14 authors at 5 institutions in 3 countries.

Chunkai WangCollege of Pharmacy, University of Nebraska Medical Center , 986125 Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Qingjie ZhaoCollege of Pharmacy, University of Nebraska Medical Center , 986125 Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Mireille VargasDepartment of Medical Parasitology and Infection Biology, Swiss Tropical Institute , Socinstrasse 57, CH-4002 Basel, Switzerland.
Jeremy O JonesDepartment of Cancer Biology, Beckman Research Institute, City of Hope National Medical Center , Duarte, California 91010, United States.
Karen L WhiteCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
David M ShacklefordCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Gong ChenCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Jessica SaundersCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Alice C F NgCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Francis C K ChiuCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Yuxiang DongCollege of Pharmacy, University of Nebraska Medical Center , 986125 Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Susan A CharmanCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Jennifer KeiserDepartment of Medical Parasitology and Infection Biology, Swiss Tropical Institute , Socinstrasse 57, CH-4002 Basel, Switzerland.
Jonathan L VennerstromCollege of Pharmacy, University of Nebraska Medical Center , 986125 Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Monash University · AUNebraska Medical Center · USSwiss Tropical and Public Health Institute · CHCity Of Hope National Medical Center · USUniversity of Nebraska Medical Center · US

Funding

Optimization of Antischistosomal ChemotypesR01AI116723 · NIAID · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI VENNERSTROM, JONATHAN L · 2015 to 2024
$6.2M
Increasing the Antischistosomal Selectivity of Aryl HydantoinsR21AI097802 · NIAID · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI VENNERSTROM, JONATHAN L · 2012 to 2013
$358k
European Research Council 614739NIAID NIH HHS R01 AI116723NIAID NIH HHS R21 AI097802
6 · The paper itself

Abstract

The aryl hydantoin 1 (Ro 13-3978) was identified in the early 1980s as a promising antischistosomal lead compound. However, this series of aryl hydantoins produced antiandrogenic side effects in the host, a not unexpected outcome given their close structural similarity to the antiandrogenic drug nilutamide. Building on the known SAR of this compound series, we now describe a number of analogs of 1 designed to maximize structural diversity guided by incorporation of substructures and functional groups known to diminish ligand-androgen receptor interactions. These analogs had calculated polar surface area (PSA), measured LogD

Indexed as

Administration, OralAnimalsDose-Response Relationship, DrugHumansHydantoinsMaleMiceMolecular StructureSchistosoma mansoniSchistosomiasisSchistosomicidesSolubilityStructure-Activity RelationshipHydantoinsSchistosomicides

Identifiers

PMID27933964
PMCPMC5150661
OpenAlexW2552448604

What OpenQuestion holds

Textmetadata
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.