Evidence map›Paper›PMID 29456113›Full record

ArticleBioorganic & medicinal chemistry2018

Design, synthesis, and evaluation of the antiproliferative activity of hydantoin-derived antiandrogen-genistein conjugates.

Alex George, Idris Raji, Bekir Cinar, Omer Kucuk, Adegboyega K Oyelere

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. 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
0.7field-weighted citation impact, top 25% 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, 10 citations in OpenAlex.

  1. Cellular and Molecular Mechanisms Modulated by Genistein in Cancer.International journal of molecular sciences · 2025
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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

5 authors at 3 institutions in 1 country.

Alex GeorgeSchool of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
Idris RajiSchool of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
Bekir CinarDepartment of Biological Sciences, The Center for Cancer Research and Therapeutic Development, Clark Atlanta University, Atlanta, GA 30314, USA.
Omer KucukWinship Cancer Institute of Emory University, Atlanta, GA 30322, USA. Electronic address: omer.kucuk@emory.edu.
Adegboyega K OyelereSchool of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA; Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA. Electronic address: aoyelere@gatech.edu.
Georgia Institute of Technology · USCenter for Cancer Research · USEmory University · US

Funding

Technologies/Resources for Core LaboratoriesG12MD007590 · NIMHD · CLARK ATLANTA UNIVERSITY · PI KHAN, SHAFIQ A · 2012 to 2018
$7.6M
Histone Deacetylase Inhibitors Equipped with Estrogen Receptor Modulation ActivitR21CA185690 · NCI · GEORGIA INSTITUTE OF TECHNOLOGY · PI OYELERE, ADEGBOYEGA · 2014 to 2015
$359k
NCI NIH HHS R21 CA185690NIMHD NIH HHS G12 MD007590
6 · The paper itself

Abstract

Androgen receptor (AR) signaling is vital to the viability of all forms of prostate cancer (PCa). With the goal of investigating the effect of simultaneous inhibition and depletion of AR on viability of PCa cells, we designed, synthesized and characterized the bioactivities of bifunctional agents which incorporate the independent cancer killing properties of an antiandrogen and genistein, and the AR downregulation effect of genistein within a single molecular template. We observed that a representative conjugate, 9b, is much more cytotoxic to both LNCaP and DU145 cells relative to the antiandrogen and genistein building blocks as single agents or their combination. Moreover, conjugate 9b more effectively down regulates cellular AR protein levels relative to genistein and induces S phase cell cycle arrest. The promising bioactivities of these conjugates warrant further investigation.

Indexed as

Drug DesignAndrogen AntagonistsAntineoplastic AgentsCell CycleCell ProliferationCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorGenisteinHumansHydantoinsMolecular StructureReceptors, AndrogenStructure-Activity RelationshipTumor Cells, CulturedAndrogen AntagonistsAntineoplastic AgentsGenisteinHydantoinsReceptors, AndrogenAndrogen receptorAntiandrogenDU145GenisteinLNCaPProstate cancer

Identifiers

PMID29456113
PMCPMC5891370
OpenAlexW2790199185

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.