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Synthesis, antimicrobial, and antiproliferative activities of substituted phenylfuranylnicotinamidines

Overview of attention for article published in Drug Design, Development and Therapy, March 2016
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2 tweeters

Citations

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14 Mendeley
Title
Synthesis, antimicrobial, and antiproliferative activities of substituted phenylfuranylnicotinamidines
Published in
Drug Design, Development and Therapy, March 2016
DOI 10.2147/dddt.s102128
Pubmed ID
Authors

Mohamed Ismail, Reem Arafa, Magdy Youssef

Abstract

This research work deals with the design and synthesis of a series of substituted phenylfuranylnicotinamidines 4a-i. Facile preparation of the target compounds was achieved by Suzuki coupling-based synthesis of the nitrile precursors 3a-i, followed by their conversion to the corresponding nicotinamidines 4a-i utilizing LiN(TMS)2. The antimicrobial activities of the newly synthesized nicotinamidine derivatives were evaluated against the Gram-negative bacterial strains Escherichia coli and Pseudomonas aeruginosa as well as the Gram-positive bacterial strains Staphylococcus aureus and Bacillus megaterium. The minimum inhibitory concentration values of nicotinamidines against all tested microorganisms were in the range of 10-20 μM. In specific, compounds 4a and 4b showed excellent minimum inhibitory concentration values of 10 μM against Staphylococcus aureus bacterial strain and were similar to ampicillin as an antibacterial reference. On the other hand, selected nicotinamidine derivatives were biologically screened for their cytotoxic activities against a panel of 60 cell lines representing nine types of human cancer at a single high dose at National Cancer Institute, Bethesda, MD, USA. Nicotinamidines showing promising activities were further assessed in a five-dose screening assay to determine their compound concentration causing 50% growth inhibition of tested cell (GI50), compound concentration causing 100% growth inhibition of tested cell (TGI), and compound concentration causing 50% lethality of tested cell (LC50) values. Structure-activity relationship studies demonstrated that the activity of members of this series can be modulated from cytostatic to cytotoxic based on the substitution pattern/nature on the terminal phenyl ring. The most active compound was found to be 4e displaying a submicromolar GI50 value of 0.83 μM, with TGI and LC50 values of 2.51 and 100 μM, respectively. Finally, the possible underlying mechanism of action of this series of compounds was investigated by determining their nuclease-like DNA degradation ability in addition to their antioxidant power and all monocations proved to be effective in all assays.

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 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 14 100%

Demographic breakdown

Readers by professional status Count As %
Professor 3 21%
Student > Doctoral Student 1 7%
Other 1 7%
Lecturer 1 7%
Lecturer > Senior Lecturer 1 7%
Other 4 29%
Unknown 3 21%
Readers by discipline Count As %
Chemistry 3 21%
Medicine and Dentistry 2 14%
Biochemistry, Genetics and Molecular Biology 1 7%
Agricultural and Biological Sciences 1 7%
Environmental Science 1 7%
Other 1 7%
Unknown 5 36%

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 16 March 2016.
All research outputs
#5,339,757
of 7,401,456 outputs
Outputs from Drug Design, Development and Therapy
#430
of 950 outputs
Outputs of similar age
#178,931
of 276,075 outputs
Outputs of similar age from Drug Design, Development and Therapy
#33
of 79 outputs
Altmetric has tracked 7,401,456 research outputs across all sources so far. This one is in the 24th percentile – i.e., 24% of other outputs scored the same or lower than it.
So far Altmetric has tracked 950 research outputs from this source. They receive a mean Attention Score of 3.2. This one is in the 47th percentile – i.e., 47% 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 276,075 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 29th percentile – i.e., 29% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 79 others from the same source and published within six weeks on either side of this one. This one is in the 48th percentile – i.e., 48% of its contemporaries scored the same or lower than it.