Evidence map›Paper›PMID 29080240›Full record

ArticleChemMedChem2017

Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Amine-based Histone Deacetylase Inhibitors.

Hazem Abdelkarim, Raghupathi Neelarapu, Antonett Madriaga, Aditya S Vaidya, Irida Kastrati, Bhargava Karumudi, Yue-Ting Wang, Taha Y Taha, Gregory R J Thatcher, Jonna Frasor and 1 more

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

Article in ChemMedChem, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.7field-weighted citation impact, top 30% 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

3 citing papers in PubMed, 13 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
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

11 authors at 1 institution in 1 country.

Hazem AbdelkarimDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Raghupathi NeelarapuDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Antonett MadriagaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Aditya S VaidyaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Irida KastratiDepartment of Physiology and Biophysics, College of Medicine, University of Illinois at Chicago, 835 South Wolcott, Chicago, IL, 60612, USA.
Bhargava KarumudiDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Yue-Ting WangDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Taha Y TahaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Gregory R J ThatcherDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Jonna FrasorDepartment of Physiology and Biophysics, College of Medicine, University of Illinois at Chicago, 835 South Wolcott, Chicago, IL, 60612, USA.
Pavel A PetukhovDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.ORCID 0000-0003-1554-242X
University of Illinois Chicago · US

Funding

Generating Human Cord-Blood-Derived Functional Megakaryocytes and platelets.R01HL130760 · NHLBI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI MAHMUD, NADIM, MILLER, WILLIAM M · 2015 to 2018
$1.7M
Photoaffinity labeling probes for development of novel isoform selective HDAC inhR01CA131970 · NCI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI PETUKHOV, PAVEL A · 2008 to 2011
$1.3M
Photoreactive histone deacetylase probes for chromatin immunoprecipitation in canR21CA183627 · NCI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI FRASOR, JONNA, PETUKHOV, PAVEL A · 2014 to 2016
$666k
NCI NIH HHS R01 CA131970NCI NIH HHS R21 CA183627NHLBI NIH HHS R01 HL130760
6 · The paper itself

Abstract

Histone deacetylases (HDACs) are promising drug targets for a variety of therapeutic applications. Herein we describe the design, synthesis, biological evaluation in cellular models of cancer, and preliminary drug metabolism and pharmacokinetic studies (DMPK) of a series of secondary and tertiary N-substituted 7-aminoheptanohydroxamic acid-based HDAC inhibitors. Introduction of an amino group with one or two surface binding groups (SBGs) yielded a successful strategy to develop novel and potent HDAC inhibitors. The secondary amines were found to be generally more potent than the corresponding tertiary amines. Docking studies suggested that the SBGs of tertiary amines cannot be favorably accommodated at the gorge region of the binding site. The secondary amines with naphthalen-2-ylmethyl, 5-phenylthiophen-2-ylmethyl, and 1H-indol-2-ylmethyl (2 j) substituents exhibited the highest potency against class I HDACs: HDAC1 IC

Indexed as

Drug DesignAminesAntineoplastic AgentsCell Line, TumorCell ProliferationCrystallography, X-RayDose-Response Relationship, DrugDrug Screening Assays, AntitumorHistone Deacetylase InhibitorsHistone DeacetylasesHumansModels, MolecularMolecular StructureStructure-Activity RelationshipAminesAntineoplastic AgentsHistone Deacetylase InhibitorsHistone Deacetylasesaminesantitumor agentsepigeneticshistone deacetylasesinhibitors

Identifiers

PMID29080240
PMCPMC5881582
OpenAlexW2765122603

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.