Evidence map›Paper›PMID 29053266›Full record

ArticleJournal of medicinal chemistry2017

Structure-Activity Relationships of New Natural Product-Based Diaryloxazoles with Selective Activity against Androgen Receptor-Positive Breast Cancer Cells.

Andrew J Robles, Shelby McCowen, Shengxin Cai, Michaels Glassman, Francisco Ruiz, Robert H Cichewicz, Stanton F McHardy, Susan L Mooberry

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed, 1 pooled it
1.8field-weighted citation impact, top 15% 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

11 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.

  1. Pooled it
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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

8 authors at 2 institutions in 1 country.

Shelby McCowenCenter for Innovative Drug Discovery, Department of Chemistry, The University of Texas at San Antonio , 1 UTSA Circle, San Antonio, Texas 78249, United States.
Shengxin Cai
Michaels GlassmanCenter for Innovative Drug Discovery, Department of Chemistry, The University of Texas at San Antonio , 1 UTSA Circle, San Antonio, Texas 78249, United States.
Francisco RuizCenter for Innovative Drug Discovery, Department of Chemistry, The University of Texas at San Antonio , 1 UTSA Circle, San Antonio, Texas 78249, United States.
Robert H CichewiczORCID 0000-0003-0744-4117
Stanton F McHardyCenter for Innovative Drug Discovery, Department of Chemistry, The University of Texas at San Antonio , 1 UTSA Circle, San Antonio, Texas 78249, United States.ORCID 0000-0003-0070-4924
Susan L Mooberry
The University of Texas at San Antonio · USThe University of Texas Health Science Center at San Antonio · US

Funding

TISSUE CULTURE---COREP30CA054174 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI Lei Zheng · 1991 to 2026
$59.1M
Recruiting and Retaining URM StudentsR25GM095480 · NIGMS · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI OYAJOBI, BABATUNDE OLUKAYODE, WEISS, DAVID S · 2011 to 2021
$3.4M
New Leads for Triple Negative Breast Cancer from Diverse Natural SourcesU01CA182740 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI CICHEWICZ, ROBERT HENRY, MOOBERRY, SUSAN L · 2014 to 2018
$2.3M
NCI NIH HHS P30 CA054174NCI NIH HHS U01 CA182740NIGMS NIH HHS R25 GM095480
6 · The paper itself

Abstract

Targeted therapies for ER+/PR+ and HER2-amplified breast cancers have improved patient survival, but there are no therapies for triple negative breast cancers (TNBC) that lack expression of estrogen and progesterone receptors (ER/PR), or amplification or overexpression of HER2. Gene expression profiling of TNBC has identified molecular subtypes and representative cell lines. An extract of the Texas native plant Amyris texana was found to have selective activity against MDA-MB-453 cells, a model of the luminal androgen receptor (LAR) subtype of TNBC. Bioassay-guided fractionation identified two oxazole natural products with selective activity against this cell line. Conducted analog synthesis and structure-activity relationship studies provided analogs with more potent and selective activity against two LAR subtype cell line models, culminating in the discovery of compound 30 (CIDD-0067106). Lead compounds discovered have potent and selective antiproliferative activities, and mechanisms of action studies show they inhibit the activity of the mTORC1 pathway.

Indexed as

Antineoplastic AgentsCell CycleCell Line, TumorDrug Screening Assays, AntitumorHumansImidazolesMechanistic Target of Rapamycin Complex 1OxazolesProlineProto-Oncogene Proteins c-aktReceptors, AndrogenRutaceaeSignal TransductionStructure-Activity RelationshipTriple Negative Breast NeoplasmsAntineoplastic AgentsCIDD-0067106ImidazolesMechanistic Target of Rapamycin Complex 1OxazolesProlineProto-Oncogene Proteins c-aktReceptors, Androgen

Identifiers

PMID29053266
PMCPMC6078197
OpenAlexW2765650189

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.