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Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A

Overview of attention for article published in European Journal of Medicinal Chemistry, January 2015
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  • Good Attention Score compared to outputs of the same age (69th percentile)
  • Good Attention Score compared to outputs of the same age and source (71st percentile)

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3 patents

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Title
Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A
Published in
European Journal of Medicinal Chemistry, January 2015
DOI 10.1016/j.ejmech.2014.12.032
Pubmed ID
Authors

Marco Pieroni, Giannamaria Annunziato, Elisa Azzali, Paola Dessanti, Ciro Mercurio, Giuseppe Meroni, Paolo Trifiró, Paola Vianello, Manuela Villa, Claudia Beato, Mario Varasi, Gabriele Costantino

Abstract

Epigenetics alterations including histone methylation and acetylation, and DNA methylation, are thought to play important roles in the onset and progression of cancer in numerous tumour cell lines. Lysine-specific demethylase 1 (LSD1 or KDM1A) is highly expressed in different cancer types and inhibiting KDM1A activity seems to have high therapeutic potential in cancer treatment. In the recent years, several inhibitors of KDM1A have been prepared and disclosed. The majority of these derivatives were designed based on the structure of tranylcypromine, as the cyclopropane core is responsible for the covalent interaction between the inhibitor and the catalytic domain of KDM proteins. In this study, we have further extended the SAR regarding compounds 1a-e, which were recently found to inhibit KDM1A with good activity. The decoration of the phenyl ring at the β-position of the cyclopropane ring with small functional groups, mostly halogenated, and in particular at the meta position, led to a significant improvement of the inhibitory activity against KDM1A, as exemplified by compound 44a, which has a potency in the low nanomolar range (31 nM).

X Demographics

X Demographics

The data shown below were collected from the profile of 1 X user 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 40 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 3%
Denmark 1 3%
Unknown 38 95%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 8 20%
Researcher 7 18%
Other 6 15%
Student > Master 3 8%
Lecturer 2 5%
Other 7 18%
Unknown 7 18%
Readers by discipline Count As %
Chemistry 18 45%
Biochemistry, Genetics and Molecular Biology 6 15%
Agricultural and Biological Sciences 4 10%
Pharmacology, Toxicology and Pharmaceutical Science 3 8%
Business, Management and Accounting 1 3%
Other 2 5%
Unknown 6 15%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 4. 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 March 2019.
All research outputs
#8,262,107
of 25,374,647 outputs
Outputs from European Journal of Medicinal Chemistry
#2,231
of 6,651 outputs
Outputs of similar age
#104,824
of 358,917 outputs
Outputs of similar age from European Journal of Medicinal Chemistry
#20
of 74 outputs
Altmetric has tracked 25,374,647 research outputs across all sources so far. This one has received more attention than most of these and is in the 66th percentile.
So far Altmetric has tracked 6,651 research outputs from this source. They receive a mean Attention Score of 4.1. This one has gotten more attention than average, scoring higher than 65% of its peers.
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 358,917 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 69% of its contemporaries.
We're also able to compare this research output to 74 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 71% of its contemporaries.