Evidence map›Paper›PMID 30140731›Full record

ArticleChemistrySelect2017

Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity.

Nicholas McConnell, Zhigang Xu, Vishnu Kumarasamy, Daekyu Sun, Brendan Frett, Hong-Yu Li

Abstract read
In one paragraph

Article in ChemistrySelect, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing 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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

6 authors.

Nicholas McConnell *Department of Pharmacology and Toxicology, University of Arizona, Tucson, Arizona 85719 United States.
Zhigang Xu *International Academy of Targeted Therapeutics and Innovation Chongqing University of Arts and Sciences, 319 Honghe Ave., Yongchuan, Chongqing 402160 China.
Vishnu KumarasamyDepartment of Pharmacology and Toxicology, University of Arizona, Tucson, Arizona 85719 United States.
Daekyu SunDepartment of Pharmacology and Toxicology, University of Arizona, Tucson, Arizona 85719 United States.
Brendan FrettDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205 United States hli2@uams.edu.
Hong-Yu LiDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205 United States hli2@uams.edu.

Funding

The Role o f Tetrahydrobiopterin (BH4) Bioavailability in Radiation-induced Skin InjuryP20GM109005 · NIGMS · UNIV OF ARKANSAS FOR MED SCIS · PI BOERMA, MARJAN · 2015 to 2024
$21.1M
CHEMISTRY-BIOLOGY INTERFACE TRAINING PROGRAMT32GM008804 · NIGMS · UNIVERSITY OF ARIZONA · PI MONTFORT, WILLIAM R. · 2003 to 2023
$3.9M
Selective RET Kinase and Its Mutant Inhibitors for the Treatment of Medullary Thyroid CancerR01CA197178 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, MCDONALD, NEIL · 2015 to 2019
$1.5M
Discovery and Development of a Selective pan-FLT3-ITD Kinase Inhibitor Clinical Candidate for the Treatment of FLT3-ITD-Driven AMLR01CA194094 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, SHAH, NEIL P · 2015 to 2018
$1.5M
Identification of Dual CSF-1R/Aurora B Kinase Inhibitors as a Novel Breast Cancer Treatment ParadigmF99CA212480 · NCI · UNIVERSITY OF ARIZONA · PI MCCONNELL, NICHOLAS MATTHEW · 2016 to 2017
$89k
NCI NIH HHS F99 CA212480NCI NIH HHS R01 CA194094NCI NIH HHS R01 CA197178NIGMS NIH HHS P20 GM109005NIGMS NIH HHS T32 GM008804
6 · The paper itself

Abstract

Benzimidazoles and quinoxalinones are present in the core of many pharmacologically relevant compounds. Several combinatorial methods have been developed to attach ring systems to both scaffolds for derivatization at select positions. Herein, we describe the development of novel constrained heterocyclic compounds attached to the N1 position of both benzimidazole and quinoxalinone scaffolds. Utilizing robust post-Ugi cyclization methods, including the Ugi-deprotection-cyclization (UDC) methodology, allows for efficient access to a new area of chemical space. Additionally, molecular modeling and in cellulo screening was employed to therapeutically validate the compounds formed with this method.

Indexed as

Heterocycle FormationMDM2/MDMXMulticomponent ReactionPost-Ugi ModificationsUgi Condensation

Identifiers

PMID30140731
PMCPMC6103208

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.