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Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A‑4

Overview of attention for article published in Journal of Medicinal Chemistry, July 2018
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Title
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A‑4
Published in
Journal of Medicinal Chemistry, July 2018
DOI 10.1021/acs.jmedchem.8b00050
Pubmed ID
Authors

Diana Lamaa, Hsin-Ping Lin, Lena Zig, Cyril Bauvais, Guillaume Bollot, Jérôme Bignon, Helene Levaique, Olivier Pamlard, Joelle Dubois, Mehdi Ouaissi, Martin Souce, Athena Kasselouri, François Saller, Delphine Borgel, Chantal Jayat-Vignoles, Hazar Al-Mouhammad, Jean Feuillard, Karim Benihoud, Mouad Alami, Abdallah Hamze

Abstract

Designing multi-target drugs has raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tubulin polymerization and HDAC activity. On the basis of 1,1-diarylethylenes (isoCA-4) and belinostat, a series of hybrid molecules was successfully designed and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization and HDAC8 leading to excellent antiproliferative activity.

X Demographics

X Demographics

The data shown below were collected from the profiles of 4 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 43 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 43 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 11 26%
Student > Master 8 19%
Researcher 3 7%
Professor > Associate Professor 2 5%
Student > Doctoral Student 1 2%
Other 4 9%
Unknown 14 33%
Readers by discipline Count As %
Chemistry 18 42%
Pharmacology, Toxicology and Pharmaceutical Science 5 12%
Agricultural and Biological Sciences 2 5%
Medicine and Dentistry 2 5%
Biochemistry, Genetics and Molecular Biology 1 2%
Other 0 0%
Unknown 15 35%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 19 July 2018.
All research outputs
#15,252,091
of 25,500,206 outputs
Outputs from Journal of Medicinal Chemistry
#20,863
of 23,197 outputs
Outputs of similar age
#181,372
of 340,369 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#120
of 162 outputs
Altmetric has tracked 25,500,206 research outputs across all sources so far. This one is in the 38th percentile – i.e., 38% of other outputs scored the same or lower than it.
So far Altmetric has tracked 23,197 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.0. This one is in the 9th percentile – i.e., 9% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 340,369 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 44th percentile – i.e., 44% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 162 others from the same source and published within six weeks on either side of this one. This one is in the 24th percentile – i.e., 24% of its contemporaries scored the same or lower than it.