Evidence map›Paper›PMID 28552339›Full record

ArticleBioorganic & medicinal chemistry letters2017

Design, synthesis and evaluation of antitumor acylated monoaminopyrroloquinazolines.

Bo Chao, Bingbing X Li, Xiangshu Xiao

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. Mechanistic insights into the activation of ester prodrugs of 666-15.Bioorganic & medicinal chemistry letters · 2020
    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

3 authors.

Bo ChaoProgram in Chemical Biology, Department of Physiology and Pharmacology, Oregon Health & Science University, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA.
Bingbing X LiProgram in Chemical Biology, Department of Physiology and Pharmacology, Oregon Health & Science University, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA.
Xiangshu XiaoProgram in Chemical Biology, Department of Physiology and Pharmacology, Oregon Health & Science University, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA; Knight Cancer Institute, Oregon Health & Science University, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA. Electronic address: xiaoxi@ohsu.edu.

Funding

Targeting Hsp60 to Inhibit CREB-mediated Gene TranscriptionR01GM122820 · NIGMS · OREGON HEALTH & SCIENCE UNIVERSITY · PI XIAO, XIANGSHU · 2017 to 2023
$1.9M
NIGMS NIH HHS R01 GM122820
6 · The paper itself

Abstract

Pyrroloquinazoline is a privileged chemical scaffold with diverse biological activities. We recently described a series of N-3 acylated 1,3-diaminopyrroloquinazolines with potent anticancer activities. The N-1 primary amino group in 1,3-diaminopyrroloquinazoline is critical for its inhibitory activity against dihydrofolate reductase (DHFR). In order to design out this unnecessary DHFR inhibition activity and further expand the chemical space associated with pyrroloquinazoline, we removed the N-1 primary amino group. In this report, we describe our design and synthesis of a series of N-3 acylated monoaminopyrroloquinazolines. Biological evaluation of these compounds identified a naphthamide 4a as a potent anticancer agent (GI

Indexed as

Drug DesignAntineoplastic AgentsCell Line, TumorCell ProliferationFolic Acid AntagonistsHumansQuinazolinesStructure-Activity RelationshipTetrahydrofolate DehydrogenaseAntineoplastic AgentsFolic Acid AntagonistsQuinazolinesTetrahydrofolate DehydrogenaseAnticancerPrivileged scaffoldPyrroloquinazolineReduction

Identifiers

PMID28552339
PMCPMC5523855

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.