Evidence map›Paper›PMID 30388878›Full record

ArticleCells2018

Antiproliferative Activity and Molecular Docking of Novel Double-Modified Colchicine Derivatives.

Urszula Majcher, Greta Klejborowska, Mahshad Moshari, Ewa Maj, Joanna Wietrzyk, Franz Bartl, Jack A Tuszynski, Adam Huczyński

Open access · goldAbstract read
In one paragraph

Article in Cells, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
2.2field-weighted citation impact, top 13% 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

13 citing papers in PubMed, 39 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. Article
  7. Article
  8. Review
  9. Photoinduced Skeletal Rearrangement ofThe Journal of organic chemistry · 2021
    Article
  10. Review
  11. Frontiers in chemistry · 2020
    Article
  12. Article
  13. 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

8 authors at 4 institutions in 3 countries.

Urszula MajcherDepartment of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614 Poznan, Poland. urszula.majcher@amu.edu.pl.
Greta KlejborowskaDepartment of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614 Poznan, Poland. greta.klejborowska@amu.edu.pl.
Mahshad MoshariDepartment of Chemistry, University of Alberta, Edmonton, AB T6G 1Z2, Canada. moshari@ualberta.ca.
Ewa MajHirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114 Wrocław, Poland. ewa.maj@iitd.pan.wroc.pl.
Joanna WietrzykHirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114 Wrocław, Poland. wietrzyk@iitd.pan.wroc.pl.ORCID 0000-0003-4980-6606
Franz BartlInstitut für Biologie, AG Biophysikalische Chemie,Humboldt Universität zu Berlin, Invalidenstr, 42, 10099 Berlin, Germany. bartlfra@cms.hu-berlin.de.
Jack A TuszynskiDepartment of Oncology, University of Alberta, Edmonton, AB T6G 1Z2, Canada. jack.tuszynski@gmail.com.
Adam HuczyńskiDepartment of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614 Poznan, Poland. adhucz@amu.edu.pl.ORCID 0000-0003-4770-215X
Adam Mickiewicz University in Poznań · PLLudwik Hirszfeld Institute of Immunology and Experimental Therapy · PLUniversity of Alberta · CAHumboldt-Universität zu Berlin · DE

Funding

Narodowe Centrum Nauki 2016/21/B/ST5/00111
6 · The paper itself

Abstract

Microtubules are tubulin polymer structures, which are indispensable for cell growth and division. Its constituent protein β-tubulin has been a common drug target for various diseases including cancer. Colchicine has been used to treat gout, but it has also been an investigational anticancer agent with a known antimitotic effect on cells. However, the use of colchicine as well as many of its derivatives in long-term treatment is hampered by their high toxicity. To create more potent anticancer agents, three novel double-modified colchicine derivatives have been obtained by structural modifications in C-4 and C-10 positions. The binding affinities of these derivatives of colchicine with respect to eight different isotypes of human β-tubulin have been calculated using docking methods. In vitro cytotoxicity has been evaluated against four human tumor cell lines (A549, MCF-7, LoVo and LoVo/DX). Computer simulations predicted the binding modes of these compounds and hence the key residues involved in the interactions between tubulin and the colchicine derivatives. Two of the obtained derivatives, 4-bromothiocolchicine and 4-iodothiocolchicine, were shown to be active against three of the investigated cancer cell lines (A549, MCF-7, LoVo) with potency at nanomolar concentrations and a higher relative affinity to tumor cells over normal cells.

Indexed as

antimitotic agentantiproliferative activitycolchicine binding site inhibitorthiocolchicineβ-tubulin affinity

Identifiers

PMID30388878
PMCPMC6262536
OpenAlexW2898841798

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.