Evidence map›Paper›PMID 18083556›Full record

ArticleBioorganic & medicinal chemistry letters2008

Inhibition of tubulin polymerization by select alkenyldiarylmethanes.

Matthew D Cullen, Taradas Sarkar, Ernest Hamel, Tracy L Hartman, Karen M Watson, Robert W Buckheit, Christophe Pannecouque, Erik De Clercq, Mark Cushman

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2008. 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. Review
  2. 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

9 authors.

Matthew D CullenDepartment of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and Purdue Cancer Center, Purdue University, West Lafayette, IN 47907, USA.
Taradas Sarkar
Ernest Hamel
Tracy L Hartman
Karen M Watson
Robert W Buckheit
Christophe Pannecouque
Erik De Clercq
Mark Cushman

Funding

Synthesis of New NNRTLs for the Treatment of AIDSR01AI043637 · NIAID · PURDUE UNIVERSITY WEST LAFAYETTE · PI CUSHMAN, MARK S · 1999 to 2005
$998k
NIAID NIH HHS R01 AI043637NIAID NIH HHS R01-AI-43637PHS HHS C06-14499
6 · The paper itself

Abstract

During studies on the alkenyldiarylmethane (ADAM) class of non-nucleoside reverse transcriptase inhibitors (NNRTIs), analogues were discovered that exhibit low micromolar and submicromolar cytotoxicities. Since the ADAMs are structurally related to the tubulin polymerization inhibitor CC-5079, a set of 14 ADAMs were tested for inhibition of tubulin polymerization in an attempt to identify the biological target responsible for their cytotoxicity. The results indicate that, overall, the ADAMs are poor inhibitors of tubulin polymerization. However, the two most cytotoxic compounds, 15 and 16, are in fact active as inhibitors of tubulin assembly with IC(50) values of 3.7+/-0.3 and 2.8+/-0.2 microM, respectively, and they both inhibit the binding of colchicine to tubulin. Both compounds were investigated for anticancer activity in the National Cancer Institute's panel of 60 human cancer cell lines, and both compounds consistently displayed submicromolar cytotoxicities with mean-graph midpoint (MGM) values of 0.31+/-0.08 and 0.47+/-0.09 microM, respectively.

Indexed as

BiopolymersCell Line, TumorDrug Screening Assays, AntitumorHIV Reverse TranscriptaseHumansMethaneReverse Transcriptase InhibitorsTubulinBiopolymersHIV Reverse TranscriptaseMethanereverse transcriptase, Human immunodeficiency virus 1Reverse Transcriptase InhibitorsTubulin

Identifiers

PMID18083556
PMCPMC2255563

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.