Evidence map›Paper›PMID 21870795›Full record

ArticleJournal of medicinal chemistry2011

Design and synthesis of (+)-discodermolide-paclitaxel hybrids leading to enhanced biological activity.

Amos B Smith, Keizo Sugasawa, Onur Atasoylu, Chia-Ping Huang Yang, Susan Band Horwitz

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Structural Basis of Microtubule Stabilization by Discodermolide.Chembiochem : a European journal of chemical biology · 2017
    Article
  6. Prodrug Strategies for Paclitaxel.International journal of molecular sciences · 2016
    Review
  7. Review
  8. Review
  9. Review
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

5 authors.

Amos B SmithDepartment of Chemistry, Monell Chemical Senses Center and Laboratory for Research on the Structure of Matter, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Keizo Sugasawa
Onur Atasoylu
Chia-Ping Huang Yang
Susan Band Horwitz

Funding

TAXOL--MECHANISMS OF ACTION AND RESISTANCER01CA077263 · NCI · YESHIVA UNIVERSITY · PI HORWITZ, SUSAN BAND, MCDAID, HAYLEY M. · 1998 to 2019
$7.8M
THE MILBEMYCINS: POTENT ANTHELMINTIC AGENTSR01GM029028 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI SMITH, AMOS B · 1985 to 2015
$4.0M
NCI NIH HHS CA-077263NCI NIH HHS R01 CA077263NIGMS NIH HHS GM-29028NIGMS NIH HHS R01 GM029028
6 · The paper itself

Abstract

Potential binding modes of (+)-discodermolide at the paclitaxel binding site of tubulin have been identified by computational studies based on earlier structural and SAR data. Examination of the prospective binding modes reveal that the aromatic pocket occupied by the paclitaxel side chain is unoccupied by (+)-discodermolide. Based on these findings, a small library of (+)-discodermolide-paclitaxel hybrids have been designed and synthesized. Biological evaluation reveals a two- to eight-fold increase in antiproliferative activity compared to the parent molecule using the A549 and MCF-7 cancer cell lines.

Indexed as

AlkanesAntineoplastic AgentsBinding SitesCarbamatesCell Line, TumorDrug DesignDrug Screening Assays, AntitumorHumansLactonesMicrotubulesModels, MolecularMolecular ConformationPaclitaxelProtein BindingPyronesSolutionsAlkanesAntineoplastic AgentsCarbamatesdiscodermolideLactonesPaclitaxelPyronesSolutionsTubulin

Identifiers

PMID21870795
PMCPMC3174350

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.