Evidence map›Paper›PMID 27614919›Full record

ArticleBioorganic & medicinal chemistry2016

Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.

Samantha M Gromek, James A deMayo, Andrew T Maxwell, Ashley M West, Christopher M Pavlik, Ziyan Zhao, Jin Li, Andrew J Wiemer, Adam Zweifach, Marcy J Balunas

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing 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

12 citing papers in PubMed.

  1. Article
  2. Synthesis and biological evaluation ofJournal of enzyme inhibition and medicinal chemistry · 2024
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  7. Review
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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

10 authors.

Samantha M GromekDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
James A deMayoDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Andrew T MaxwellDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Ashley M WestDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Christopher M PavlikDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Ziyan ZhaoDepartment of Molecular and Cell Biology, University of Connecticut, 91 N. Eagleville Rd, Storrs, CT 06269, USA.
Jin LiDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Andrew J WiemerDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA.
Adam ZweifachDepartment of Molecular and Cell Biology, University of Connecticut, 91 N. Eagleville Rd, Storrs, CT 06269, USA.
Marcy J BalunasDivision of Medicinal Chemistry, Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd, Storrs, CT 06269, USA. Electronic address: marcy.balunas@uconn.edu.

Funding

Resource for Biocomputing Visualization and InformaticsP41GM103311 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI FERRIN, THOMAS E · 2012 to 2017
$8.2M
ICBG: "Training, Conservation and Drug Discovery using Panamanian MicroorganismsU01TW006634 · FIC · SMITHSONIAN INSTITUTION · PI GERWICK, WILLIAM HENRY · 2003 to 2013
$7.8M
Tropical Disease Drug Discovery from Marine Cyanobacteria in PanamaK01TW008002 · FIC · UNIVERSITY OF CONNECTICUT STORRS · PI BALUNAS, MARCY J · 2009 to 2011
$246k
FIC NIH HHS K01 TW008002FIC NIH HHS U01 TW006634NIGMS NIH HHS P41 GM103311
6 · The paper itself

Abstract

Santacruzamate A (SCA) is a natural product isolated from a Panamanian marine cyanobacterium, previously reported to have potent and selective histone deacetylase (HDAC) activity. To optimize the enzymatic and cellular activity, 40 SCA analogues were synthesized in a systematic exploration of the zinc-binding group (ZBG), cap terminus, and linker region. Two cap group analogues inhibited proliferation of MCF-7 breast cancer cells, with analogous increased degranulation of cytotoxic T cells (CTLs), while one cap group analogue reduced CTL degranulation, indicative of suppression of the immune response. Additional testing of these analogues resulted in reevaluation of the previously reported SCA mechanism of action. These analogues and the resulting structure-activity relationships will be of interest for future studies on cell proliferation and immune modulation.

Indexed as

Antineoplastic AgentsCarbamatesCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMCF-7 CellsMolecular StructureStructure-Activity RelationshipT-Lymphocytes, CytotoxicAntineoplastic AgentsCarbamatessantacruzamate AAnti-proliferative activityEnzyme assaysImmune modulationNatural product analoguesSantacruzamate A

Identifiers

PMID27614919
PMCPMC5065774

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.