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A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin

Overview of attention for article published in Bioorganic & Medicinal Chemistry, July 2016
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Mentioned by

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2 tweeters

Citations

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9 Dimensions

Readers on

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19 Mendeley
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Title
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin
Published in
Bioorganic & Medicinal Chemistry, July 2016
DOI 10.1016/j.bmc.2016.05.043
Pubmed ID
Authors

Jelica Vucicevic, Tatjana Srdic-Rajic, Marco Pieroni, Jonne M.M. Laurila, Vladimir Perovic, Sabrina Tassini, Elisa Azzali, Gabriele Costantino, Sanja Glisic, Danica Agbaba, Mika Scheinin, Katarina Nikolic, Marco Radi, Nevena Veljkovic

Abstract

The clonidine-like central antihypertensive agent rilmenidine, which has high affinity for I1-type imidazoline receptors (I1-IR) was recently found to have cytotoxic effects on cultured cancer cell lines. However, due to its pharmacological effects resulting also from α2-adrenoceptor activation, rilmenidine cannot be considered a suitable anticancer drug candidate. Here, we report the identification of novel rilmenidine-derived compounds with anticancer potential and devoid of α2-adrenoceptor effects by means of ligand- and structure-based drug design approaches. Starting from a large virtual library, eleven compounds were selected, synthesized and submitted to biological evaluation. The most active compound 5 exhibited a cytotoxic profile similar to that of rilmenidine, but without appreciable affinity to α2-adrenoceptors. In addition, compound 5 significantly enhanced the apoptotic response to doxorubicin, and may thus represent an important tool for the development of better adjuvant chemotherapeutic strategies for doxorubicin-insensitive cancers.

Twitter Demographics

The data shown below were collected from the profiles of 2 tweeters who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 19 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 19 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 2 11%
Researcher 2 11%
Student > Ph. D. Student 2 11%
Professor 2 11%
Unspecified 1 5%
Other 5 26%
Unknown 5 26%
Readers by discipline Count As %
Chemistry 6 32%
Biochemistry, Genetics and Molecular Biology 3 16%
Pharmacology, Toxicology and Pharmaceutical Science 2 11%
Arts and Humanities 1 5%
Medicine and Dentistry 1 5%
Other 0 0%
Unknown 6 32%

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 27 May 2016.
All research outputs
#7,291,904
of 12,272,194 outputs
Outputs from Bioorganic & Medicinal Chemistry
#4,230
of 5,113 outputs
Outputs of similar age
#136,596
of 275,963 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry
#20
of 65 outputs
Altmetric has tracked 12,272,194 research outputs across all sources so far. This one is in the 39th percentile – i.e., 39% of other outputs scored the same or lower than it.
So far Altmetric has tracked 5,113 research outputs from this source. They receive a mean Attention Score of 4.0. This one is in the 17th percentile – i.e., 17% 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 275,963 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 49th percentile – i.e., 49% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 65 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 70% of its contemporaries.