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Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors

Overview of attention for article published in European Journal of Medicinal Chemistry, November 2015
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Title
Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors
Published in
European Journal of Medicinal Chemistry, November 2015
DOI 10.1016/j.ejmech.2015.11.010
Pubmed ID
Authors

Florian Thaler, Loris Moretti, Raffaella Amici, Agnese Abate, Andrea Colombo, Giacomo Carenzi, Maria Carmela Fulco, Roberto Boggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci, Luca Sartori, Mario Varasi, Ciro Mercurio

Abstract

In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4'-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 22 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 22 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 7 32%
Other 3 14%
Student > Bachelor 2 9%
Student > Doctoral Student 2 9%
Researcher 2 9%
Other 4 18%
Unknown 2 9%
Readers by discipline Count As %
Chemistry 10 45%
Biochemistry, Genetics and Molecular Biology 3 14%
Agricultural and Biological Sciences 2 9%
Environmental Science 1 5%
Unknown 6 27%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. 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 15 December 2015.
All research outputs
#22,759,452
of 25,374,647 outputs
Outputs from European Journal of Medicinal Chemistry
#5,701
of 6,651 outputs
Outputs of similar age
#250,924
of 293,335 outputs
Outputs of similar age from European Journal of Medicinal Chemistry
#61
of 84 outputs
Altmetric has tracked 25,374,647 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,651 research outputs from this source. They receive a mean Attention Score of 4.1. This one is in the 1st percentile – i.e., 1% 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 293,335 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 84 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.